Payload ID	PAY0FSXOW
Name	Monomethyl auristatin E
Synonyms	Monomethyl auristatin E; 474645-27-7; MMAE; Monomethylauristatin E; MMAE (Monomethyl auristatin E); V7I58RC5EJ; SGD-1010; (2S)-N-[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamide; N-Methyl-L-valyl-N-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1-methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-L-valinamide; MMAE peptide; N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide; UNII-V7I58RC5EJ; Monomethyl auristatin E (MMAE); MFCD22124498; 4Q5; MMAE, monomethyl auristatin E; SCHEMBL5402144; CHEMBL2103835; AMY9235; DTXSID101028844; MONOMETHYLAURISTATIN E [MI]; (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1R,2R)-1-Hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxohe; n-methyl-l-valyl-n-[(1s,2r)-4-[(2s)-2-[(1r,2r)-3-[[(1r,2s)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-n-methyl-l-valinamide; FD9056; NSC791792; NSC832263; s7721; CCG-270400; CS-0837; NSC-791792; NSC-832263; BP-22278; HY-15162; Q6901739; (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-Hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide; L-Valinamide, N-methyl-L-valyl-N-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1- methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)-1-pyrrolidinyl)-2- methoxy-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-; N(sup 2)-(N-Methyl-L-valyl)-N(sup 1)-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1-methyl-2- phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1S)- 1-methylpropyl)-4-oxobutyl)-N(sup 1)-methyl-L-valinamide    Click to Show/Hide
Target(s)	Microtubule (MT)					Target Info
Structure
	3D MOL			2D MOL
Formula	C39H67N5O7
Isosmiles	CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@H](C)[C@H](C2=CC=CC=C2)O)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC
PubChem CID	11542188
InChI	InChI=1S/C39H67N5O7/c1-13-25(6)34(43(10)39(49)33(24(4)5)42-38(48)32(40-9)23(2)3)30(50-11)22-31(45)44-21-17-20-29(44)36(51-12)26(7)37(47)41-27(8)35(46)28-18-15-14-16-19-28/h14-16,18-19,23-27,29-30,32-36,40,46H,13,17,20-22H2,1-12H3,(H,41,47)(H,42,48)/t25-,26+,27+,29-,30+,32-,33-,34-,35+,36+/m0/s1
InChIKey	DASWEROEPLKSEI-UIJRFTGLSA-N
IUPAC Name	(2S)-N-[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamide
Pharmaceutical Properties	Molecule Weight		718	Polar area		150
	Complexity		1100	xlogp Value		4.1
	Heavy Count		51	Rot Bonds		20
	Hbond acc		8	Hbond Donor		4

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.13±0.02	nM	MDA-MB-231 cells	Breast adenocarcinoma	CVCL_0062	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.25	nM	Granta-519 cells	Mantle cell lymphoma	CVCL_1818	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.25	nM	SU-DHL-4 cells	Diffuse large B-cell lymphoma	CVCL_0539	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.54	nM	BJAB cells	Burkitt lymphoma	CVCL_5711	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.66±0.06	nM	MDA-MB-468 cells	Breast adenocarcinoma	CVCL_0419	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	1.19	nM	SU-DHL-4 cells	Diffuse large B-cell lymphoma	CVCL_0539	[1], [2]

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Two-year Progression-Free Survival (PFS)	97.30% (BV-AVD group); 92.60% (ABVD group)
Patients Enrolled	34 patients with previously untreated classical Hodgkin lymphoma (cHL).
Administration Dosage	After 2 cycles of Brentuximab vedotin, doxorubicin, dacarbazine combination therapy.
Related Clinical Trial
NCT Number	NCT02505269	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin plus ad in non-bulky limited stage Hodgkin lymphoma.
Primary Endpoint	For patients with high total metabolic tumor volume, the 2-year PFS rate was 90.90% and 70.70% in the BV-AVD and ABVD arms, respectively. 82.30% in the BV-AVD arm were PET-negative compared with 75.40% in the ABVD arm.
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Objective Response Rate (ORR)	59.00%
Patients Enrolled	Eastern Cooperative Oncology Group performance status 2 with previously untreated CD30-positive PTCL (CD30 detected in 10% of neoplastic cells by local review.
Administration Dosage	Patients were treated with six or eight 21-day cycles of either brentuximab vedotin, cyclophosphamide, doxorubicin, prednisone (A+CHP) or cyclophosphamide, doxorubicin, vincristine, prednisone (CHOP).
Related Clinical Trial
NCT Number	NCT01777152	Phase Status	Phase 3
Clinical Description	A randomized, double-blind, placebo-controlled, phase 3 study of brentuximab vedotin and CHP (A+CHP) versus CHOP in the frontline treatment of patients with CD30-positive mature T-cell lymphomas.
Primary Endpoint	The median PFS = 62.30 months (95% CI: 42.00 months to not evaluable) for A+CHP. The median PFS = 23.80 months (95% CI: 13.60-60.80 months) for CHOP.
Other Endpoint	5-year overall survival (OS) rates = 70.10% (95% CI: 63.30% to 75.90%) with A+CHP VS 61.00% (95% CI: 54.00% to 67.30%) with CHOP (hazard ratio = 0.72; 95% CI: 0.53-0.99), The PFS HR = 0.55 (95% CI: 0.39-0.79; P = 0.0009) in the subset of patients with sALCL, and the estimated 5-year PFS = 60.60% (95% CI: 49.50% to 69.90%) for A+CHP,the estimated 5-year PFS= 48.40% (95% CI: 39.60% to 56.70%) for CHOP The ORR with first subsequent therapy on the A+CHP arm = 42.00% (27.00% CR) VS The ORR with first subsequent therapy = 42.00% (19.00% CR) in the CHOP armCR=72.57% (82/113) in the A+CHP arm were in CR at EOT, and = 30.49% (25/82) underwent consolidative SCT.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Objective Response Rate (ORR)	60.00%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	Relapsed or progressive Hodgkin lymphoma (HL).
Administration Dosage	1.8 mg/kg IV once every 3 weeks for up to 16 cycles.
Related Clinical Trial
NCT Number	NCT01100502	Phase Status	Phase 3
Clinical Description	A phase 3 study of brentuximab vedotin (SGN-35) in patients at high risk of residual Hodgkin lymphoma following stem cell transplant (the AETHERA trial).
Primary Endpoint	Objective response rate=60.00% (including 4 complete responses, 2 partial responses, 1 stable disease, 1 progressive disease, and 2 unknown).
Other Endpoint	5-year PFS=59.00% (95% CI 51.00-66.00).
Experiment 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Objective Response Rate (ORR)	60.13%
Patients Enrolled	Elapsed or refractory classical Hodgkin lymphoma with measurable disease and an Eastern Cooperative Oncology Group performance status of 0 or 1 who were ineligible for or had relapsed after autologous haematopoietic stem-cell transplantation (HSCT).
Administration Dosage	1.80 mg/kg intravenously every 3 weeks.
Related Clinical Trial
NCT Number	NCT02684292	Phase Status	Phase 3
Clinical Description	A phase 3, randomized, open-label, clinical trial to compare pembrolizumab with brentuximab vedotin in subjects with relapsed or refractory classical hodgkin lymphoma.
Primary Endpoint	Median progression-free survival = 13.20 months (95% CI 10.90-19.40) for pembrolizumab vs median progression-free survival = 8.30 months (5.70-8.80) for brentuximab vedotin (hazard ratio 0.65 [95% CI 0.48-0.88].; p=0.0027).
Other Endpoint	Objective responses (by investigator review) were recorded in 103 (68.21% [95% CI 60.1-75.5]) of 151 patients in the pembrolizumab group (40 [26.48%] complete responses and 63 [41.72%] partial responses), and in 92 (60.13% [51.9-67.9]) of 153 patients in the brentuximab vedotin group (36 [23.53%] complete responses and 56 [36.60%] partial responses).    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Objective Response Rate (ORR)	0.00%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	Histologically confirmed diagnoses of advSM (ASM, SM-AHN, or MCL).
Administration Dosage	1.8 mg/kg IV every 3 weeks up to 8 cycles.
Related Clinical Trial
NCT Number	NCT01807598	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin in treating patients with advanced systemic mastocytosis or mast cell leukemia.
Primary Endpoint	Objective response rate=0.00%.
Other Endpoint	Median progression-free survival=210 days (95% CI 77-343 days).
Experiment 6 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Objective Response Rate (ORR)	8.00%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	CD30-expressing nonlymphomatous cancer, not have been treated with chemotherapy, radiotherapy, biologics.
Administration Dosage	1.8 or 2.4 mg/kg BV once every three weeks.
Related Clinical Trial
NCT Number	NCT01461538	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin in patients with CD30-positive nonlymphomatous malignancies.
Primary Endpoint	Objective response rate= 8.00% (95% CI 1.10, 28.00).
Other Endpoint	Median progression-free survival=2.10 months (95% CI 1.20- 2.80).
Experiment 7 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Objective Response Rate (ORR)	13.33%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Patients Enrolled	Relapsed/refractory CD30+ primary mediastinal large B-cell lymphoma (PmLBCL).
Administration Dosage	1.80 mg per kg as a single IV infusion on day 1 of each 21-day cycle.
Related Clinical Trial
NCT Number	NCT02423291	Phase Status	Phase 2
Clinical Description	A phase 2 study of SGN-35 (Brentuximab Vedotin) of patients with relapsed or refractory primary mediastinal large B-cell lymphoma (PmLBCL).
Primary Endpoint	The ORR was 13.33% (2/15): 2 patients PR, 1 patient SD, and the remaining 12 patients PD.
Experiment 8 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Objective Response Rate (ORR)	36.40%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Patients Enrolled	Any subtype of histologically confirmed high-CD30expressing non Hodgkin lymphoma (NHL), except anaplastic large-cell lymphoma (ALCL). High CD30 expression was defined as membranous CD30 expression in 30% of tumor cells detectable by visual assessment of routine immunohistochemistry staining using the anti-CD30 antibody on biopsy at the time of diagnosis or relapse. (2) A bidimensionally measurable lesion 1.5 cm in the greatest transverse diameter. (3) Age 20-75 years and an Eastern Cooperative Oncology Group performance status of 2. (4) Adequate bone marrow and organ function. (5) No history of another active cancer within the previous 5 years except basal cell carcinoma. Note that patients who had relapsed after autologous stem cell transplantation (SCT) were considered eligible. Exclusion criteria were: undergoing allogeneic SCT; active infection, human immunodeficiency virus infection, or hepatitis B or C; and lymphomatous involvement of the central nervous system. The 30% cutoff was established by consensus during an investigation initiation meeting of the pathologists from each of the study sites after they reviewed various cutoff values for positive and strong positive of CD30 expression across various subtypes of NHL.    Click to Show/Hide
Administration Dosage	Intravenously at 1.80 mg/kg every 3 weeks and the primary endpoint was > 40% disease control rate.
Related Clinical Trial
NCT Number	NCT02280785	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin for relapsed/refractory CD30-positive non-Hodgkin lymphomas other than anaplastic large cell lymphoma.
Primary Endpoint	For 1.80 mg/kg BV intravenously, the overall disease control rate was 48.48% (16/33).
Other Endpoint	For 1.80 mg/kg BV intravenously, the median PFS and OS 1.90 months and 6.10 months.
Experiment 9 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Objective Response Rate (ORR)	41.18% (In 34 evaluable patients) 54.00% (AITL)
Patients Enrolled	Relapsed/refractory CD30+ non-Hodgkin lymphomas; at least 1 prior systemic therapy, measurable disease, age 12 years, and Eastern Cooperative Oncology Group (ECOG) performance status of 2.
Administration Dosage	1.80 mg/kg was administered every 3 weeks until progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT01421667	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin in relapsed or refractory non-hodgkin lymphoma (NHL).
Primary Endpoint	In 34 evaluable patients, ORR was 41.18% (8 CRs, 6 PRs,and ORR was 54.00% in AITL (5 CRs, 2 PRs) with median PFS of 6.70 months thus far.
Other Endpoint	Median baseline sCD30 for patients with AITL and PTCL-NOS was 1214 ng/mL (range, 108-9473 ng/mL) and 840 ng/mL, respectively. Median duration of response for all patients was 7.60 months (range, 1.30-14.10 months), 5.50 months for AITL patients,and 7.60 months (range, 1.40-10.11 months) for PTCL-NOS patients.
Experiment 10 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Objective Response Rate (ORR)	48.00%	Positive CD30 expression (CD30+++/++; FACS analysis = 495)
Patients Enrolled	EBV-positive and CD30- positive non-Hodgkin lymphomas with various levels of CD30 in the relapsed or refractory setting.
Administration Dosage	1.80 mg/kg brentuximab vedotin intravenously every 3 weeks for up to 16 cycles or until disease progression.
Related Clinical Trial
NCT Number	NCT02388490	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin in patients with relapsed or refractory EBV-and CD30-positive lymphomas.
Primary Endpoint	For 1.80 mg/kg BV intravenously, the ORR was 48.00% (90% CI: 31.00%-64.00%).
Other Endpoint	For 1.80 mg/kg BV intravenously, Median Progression-Free Survival (mPFS)= 6.20 months (95% CI: 2.90-13.60), overall survival(mOS)=15.70 months (95% CI: 6.10-not reached).
Experiment 11 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Objective Response Rate (ORR)	52.94%	Positive CD30 expression (CD30+++/++; FACS analysis = 116)
Patients Enrolled	Elderly patients with relapsed/refractory Hodgkin lymphoma (R/R HL).
Administration Dosage	1.80 mg/kg administered as a single outpatient intravenous infusion on Day 1 of each 21-day treatment cycle, for a maximum of 16 cycles.
Related Clinical Trial
NCT Number	NCT02227433	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin (BV) in the treatment of elderly Hodgkin lymphoma (HL) patients at first relapse or with primary refractory disease.
Primary Endpoint	The efficacy of single agent BV was measured by overall objective response rate (ORR, sum of CR and partial response [PR] rates),Best response was reached at fourth cycle of BV therapy. ORR was 52.94% (9 of 17 patients) with a CR rate of 23.5% (4 of 17 patients).
Other Endpoint	Secondary endpoints were CR rate, disease free survival (DFS), 1-year PFS, 1-year OS and safety and tolerability of BV. With a median follow-up of 24.90 months, median PFS was 8.80 months and median OS was 21.70 months.
Experiment 12 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Objective Response Rate (ORR)	67.86% (HL and systemic ALCL retreatment patients) 60.00% (HL patients) 87.50% (systemic ALCL patients)
Patients Enrolled	Patients who previously experienced a CR or PR with brentuximab vedotin, discontinued treatment while in remission, and subsequently experienced disease progression or relapse. Patients who received an allogeneic stem cell transplant (SCT) were eligible if they were >100 days from transplant and had no evidence of cytomegalovirus by polymerase chain reaction.    Click to Show/Hide
Administration Dosage	1.80 mg/kg intravenously approximately every 3 weeks over 30 minutes as an outpatient infusion.
Related Clinical Trial
NCT Number	NCT00947856	Phase Status	Phase 2
Clinical Description	Treatment with SGN-35 in patients with CD30-positive hematologic malignancies who have previously participated in an SGN-35 study.
Primary Endpoint	The ORR for HL and systemic ALCL retreatment patients was 67.86% (95% CI; 47.60-84.10),with a CR rate of 39.29% (95% CI; 21.50-59.40). The ORR was 60.00% (30.00% CR) for HL patients and 87.50% (62.50% CR) for systemic ALCL patients. The majority of patients (81.00%) who received brentuximab vedotin retreatment experienced reduction in measurable tumor volume.    Click to Show/Hide
Other Endpoint	The objective response rate = 60.00% (30.00% CR) in HL patients and 87.50% (62.50% CR) in systemic ALCL patients.
Experiment 13 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Objective Response Rate (ORR)	71.00%
Patients Enrolled	Relapsed or refractory Hodgkin lymphoma (HL) after auto-stem cell transplant.
Administration Dosage	1.80 mg/kg IV once every 3 weeks over 30 minutes on an outpatient basis for up to 16 infusions.
Related Clinical Trial
NCT Number	NCT00848926	Phase Status	Phase 2
Clinical Description	A pivotal study of SGN-35 in treatment of patients with relapsed or refractory hodgkin lymphoma (HL).
Primary Endpoint	OrR = 72.00% (33.00% CR, 38.00% PR).
Other Endpoint	The estimated median DOR of PR in the 73 patients= 11.20 months (95% CI: 7.70, 18.70), The median DOR of CR in the 34 patients = not been reached (95% CI: 20.50 - NA months). The estimated median OS for all patients was 40.50 months (95% CI: 28.70-NA ). The estimated 3-year OS for the 34 patients with a CR to brentuximab vedotin was 73.00% (95% CI: 57%, 88%). The estimated median PFS for all patients was 9.30 months (95% CI: 7.10, 12.20). Three-year PFS was estimated at 58.00% (95% CI: 41.00%, 76.00%) for the 34 CR patients.    Click to Show/Hide
Experiment 14 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Objective Response Rate (ORR)	75.00%
Patients Enrolled	Relapsed or refractory Hodgkin lymphoma (HL) after high-dose chemotherapy and auto-stem cell transplant, histologically documented CD30-positive Hodgkin's Reed-Sternberg cells by central pathology review.
Administration Dosage	1.80 mg/kg by intravenous infusion every 3 weeks; received a maximum of 16 cycle.
Related Clinical Trial
NCT Number	NCT00848926	Phase Status	Phase 2
Clinical Description	A pivotal study of SGN-35 in treatment of patients with relapsed or refractory hodgkin lymphoma (HL).
Primary Endpoint	Tumor reductions were observed in 94% of patients. The ORR was 75.00% (95% CI, 64.90% to 82.60%); 34% of all patients achieved a CR (95% CI, 25.20% to 44.40%), and the overall disease control rate (CR + partial remission + stable disease) was 96% (95% CI, 90.30% to 98.90%). The median time to objective response was 5.70 weeks (range, 5.10 to 56 weeks),and the median time to CR was 12 weeks (range, 5.10 to 56 weeks).    Click to Show/Hide
Other Endpoint	For patients who had an objective response,the median duration of response was 6.70 months (95% CI,3.60 to 14.80 months). The median duration of response for patients who achieved a CR was 20.50 months (95% CI,10.80 months to not estimable).
Experiment 15 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Objective Response Rate (ORR)	86.00%
Patients Enrolled	Relapsed or refractory systemic anaplastic large cell lymphoma (ALCL) after treatment failure of at least one prior therapy with curative intent, the most common being a combination of cyclophosphamide, doxorubicin, vincristine, and prednisone.
Administration Dosage	1.80 mg/kg was administered intravenously once every 3 weeks over 30 minutes on an outpatient basis for up to 16 total doses.
Related Clinical Trial
NCT Number	NCT00866047	Phase Status	Phase 2
Clinical Description	A phase 2 study of SGN-35 in treatment of patients with relapsed or refractory systemic anaplastic large cell lymphoma (ALCL).
Primary Endpoint	The ORR per independent review was 86.00% (95% CI,74.60% to 93.90%); 57% of patients achieved CR (95% CI, 43.20% to 69.80%), and 29.00% achieved partial remission. Tumor reductions were observed in 97.00% of patients.
Other Endpoint	The estimated median PFS time per independent review was 13.30 months (95% CI,6.90 months to NE); in the subset of patients who achieved a CR,the median PFS was 14.60 months. Per investigator assessment,the median PFS with brentuximab vedotin was 14.30 months (95% CI,9.10 months to NE). The median OS had not yet been reached. The estimated 12-month survival rate was 70.00%.    Click to Show/Hide
Experiment 16 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Objective Response Rate (ORR)	92.31%
Patients Enrolled	Patients were aged 60 years with classical HL (ie, patients with nodular lymphocyte predominant HL [NLPHL] were excluded). Patients were treatment nave and were either ineligible for frontline conventional combination treatment of HL (eg, ABVD or bleomycin, etoposide, doxorubicin, cyclophosphamide, vincristine, procarbazine, and prednisone [BEACOPP]) in the investigators judgment or had declined the available chemotherapy options after being informed of the potential benefits and risks.    Click to Show/Hide
Administration Dosage	1.80 mg/kg of IV brentuximab vedotin every 3 weeks for up to 16 doses.
Related Clinical Trial
NCT Number	NCT01716806	Phase Status	Phase 2
Clinical Description	A phase 2 open-label study of brentuximab vedotin in front-line therapy of Hodgkin lymphoma (HL) an dCD30-expressing peripheral t-cell lymphoma (PTCL) in older patients or patients with significant comorbidities ineligible for standard chemotherapy.
Primary Endpoint	The ORR among the 26 efficacy-evaluable patients was 92.31% (n=24, 95% CI 74.90-99.10). The median duration of objective response was 9.10 months (range 2.80-20.90 months) for all responder.
Other Endpoint	The CR among the 26 efficacy-evaluable patients was 73.08% (n=19, 95% CI 52.20-88.40), The median PFS was 10.50 months (range 2.61-22.31 months) for all efficacy evaluable patients and 11.80 months (range 4.10-22.31months) for CR.
Experiment 17 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Objective Response Rate (ORR)	100.00% (for efficacy-evaluable patients treated with BV plus DTIC)
Patients Enrolled	Had treatment-naive classical HL (excluding nodular lymphocyte predominant HL), fluorodeoxyglucose positron emission tomography (PET)-avid disease, bidimensional measurable disease of >=1.5 cm in the greatest transverse diameter, and an ECOG performance status of <=3 and were ineligible for or declined standard frontline chemotherapies (eg, ABVD or bleomycin, etoposide, Adriamycin, cyclophosphamide, Oncovin, procarbazine, and prednisone).    Click to Show/Hide
Administration Dosage	1.80 mg/kg BV and 375 mg/m2 DTIC for up to 12 cycles, and 20 more patients received 1.80 mg/kg BV plus 90 or 70 mg/m2 bendamustine for up to 6 cycles (dose reduced due to toxicity).
Related Clinical Trial
NCT Number	NCT01716806	Phase Status	Phase 2
Clinical Description	A phase 2 open-label study of brentuximab vedotin in front-line therapy of hodgkin lymphoma (HL) an dCD30-expressing peripheral t-cell lymphoma (PTCL) in older patients or patients with significant comorbidities ineligible for standard chemotherapy.
Primary Endpoint	For efficacy-evaluable patients treated with BV plus DTIC (n = 21), the ORR was 100.00%. For efficacy-evaluable patients treated with BV plus bendamustine (n = 17), the ORR was also 100.00%.
Other Endpoint	For efficacy-evaluable patients treated with BV plus DTIC (n = 21), the CR rate was 62.00%. At the time of this analysis, the median observation time from first dose was 21.60 months (range, 14.80 to 29.00 months), and median PFS was 17.90 months (range, 4.20 to 29.00 months). For efficacy-evaluable patients treated with BV plus bendamustine (n = 17), the CR was also 88.00%. Out of 7 patients (57.00%) with B symptoms at baseline had resolution. The median observation time from first dose was 10.80 months (range, 2.90 to 18.20 months). Neither the median PFS (range, 2.90 to 18.00 months) nor the median OS (range, 2.90 to 18.20 months) was reached at the time of this analysis.    Click to Show/Hide
Experiment 18 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Objective Response Rate (ORR)	100.00%	High CD30 expression (CD30+++)
Patients Enrolled	35 patients with R/R Hodgkin lymphoma (HL).
Administration Dosage	Any time before on-protocol consolidation (nivolumab + BV; BV + bendamustine).
Related Clinical Trial
NCT Number	NCT02927769	Phase Status	Phase 2
Clinical Description	Risk-based, response-adapted, phase II open-label trial of nivolumab + brentuximab vedotin (N + BV) for children, adolescents, and young adults with relapsed/refractory (R/R) CD30 + classic hodgkin lymphoma (cHL) after failure of first-line therapy, followed by brentuximab + bendamustine (BV + B) for participants with a suboptimal response (checkmate 744: checkpoint pathway and nivolumab clinical trial evaluation)    Click to Show/Hide
Experiment 19 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Objective Response Rate (ORR)	100.00%	Positive CD30 expression (CD30 +++/++)
Patients Enrolled	Patients with previously untreated, early-stage unfavorable Hodgkin lymphoma.
Administration Dosage	Patients were randomly assigned (2:1) to four cycles of BV-AVD or standard doxorubicin, bleomycin, vincristine, and dacarbazine (ABVD), followed by 30 Gy involved node radiotherapy.
Related Clinical Trial
NCT Number	NCT02292979	Phase Status	Phase 2
Clinical Description	Brentuximab vedotin associated with chemotherapy in untreated patients with stage I/II unfavourable hodgkin lymphoma. a randomized phase ii lysa-fil-eortc intergroup study.
Primary Endpoint	CRR was 94.12% (32/34).
Other Endpoint	ORR was 100.00% (34/34).
Experiment 20 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Objective Response Rate (ORR)	60.71% (in the Phase 1) 78.38% (in the Phase 2)
Patients Enrolled	Relapsed/refractory CD30+ biopsy proven Hodgkin lymphoma (HL) or anaplastic large cell lymphoma (ALCL) and an ECOG Performance Status 2.
Administration Dosage	Bv was escalated from 1.20 mg/kg Day 1, and B from 70 mg/m2 Days 1 and 2 every 21 days until the MTD or recommended phase 2 dose (RP2D) was reached;Bv escalating to a dose of 1.80 mg/kg and B was escalated to 90 mg/m2.
Related Clinical Trial
NCT Number	NCT01657331	Phase Status	Phase 1/2
Clinical Description	A phase 1/2 clinical trial of the combination of brentuximab vedotin and bendamustine in patients with relapsed or refractory hodgkin lymphoma or anaplastic large cell lymphoma.
Primary Endpoint	The MTD was not reached, based on the fact there was no maximum administrable dose identified. The RP2D was Bv at 1.80 mg/kg and B at 9.00 mg/kg. Only 1 of 11 patients qualified as a DLT (Grade 4 neutropenia) at the RP2D.
Other Endpoint	17 of 28 (ORR 60.71%, 95% CI 41.00-79.00) of patients achieved a response in the Phase 1, with 5 of 28 (17.86%) being CR. In the Phase 2, 29 of 37 (ORR 78.38%, 95% CI 62.00-91.00) patients responded, with 16 of 37 (43.24%) attaining a CR.
Experiment 21 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Objective Response Rate (ORR)	50.00%	Positive CD30 expression (CD30+++/++; FACS analysis = 102)
Patients Enrolled	Patients had relapsed or refractory, histologically confirmed CD30-positive hematologic cancers. Patients with Hodgkin's lymphoma had received systemic chemotherapy either as induction therapy for advanced-stage disease or salvage therapy after initial radiotherapy for early-stage disease and had previously undergone autologous stem cell transplant (ASCT).    Click to Show/Hide
Administration Dosage	Intravenously at doses of 0.10 to 3.60 mg per kilogram of body weight every 3 weeks (one cycle).
Related Clinical Trial
NCT Number	NCT00430846	Phase Status	Phase 1
Clinical Description	A phase 1 dose escalation study of SGN-35 in patients with relapsed/refractory CD30-positive hematologic malignancies.
Primary Endpoint	Safety profile of brentuximab vedotin =1.80 mg/kg.
Other Endpoint	Secondary objectives were to determine pharmacokinetic measures for the antibody-drug conjugate and MMAE, evaluate immunogenicity, and assess antitumor response.The median time to maximum concentration occurred immediately after infusion for the antibody-drug conjugate and approximately 2 to 3 days after infusion for MMAE. Steady-state pharmacokinetics for both the antibody-drug conjugate and MMAE occurred by approximately 21 days,consistent with the half-life estimates of 4 to 6 days and 3 to 4 days, respectively.    Click to Show/Hide
Experiment 22 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Objective Response Rate (ORR)	73.00% (at a median follow-up of 11.1 months) 70.00% (BICR-assessed)
Patients Enrolled	R/R PMBL; had an Eastern Cooperative Oncology Group performance status of 0 to 1, had a CD30 expression level of 1% or greater in the tumor or tumor-infiltrating lymphocytes by local immunohistochemistry, and had 1 or more measurable sites of disease according to the Lugano 2014 classification.
Administration Dosage	Received nivolumab (240 mg intravenously) and BV (1.80 mg/kg intravenously) every 3 weeks until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02581631	Phase Status	Phase 1
Clinical Description	A phase 1/ 2 study to evaluate the safety and preliminary efficacy of nivolumab in combination with brentuximab vedotin in subjects with relapsed refractory non hodgkin lymphomas with CD30 expression (checkmate 436: CHECK point pathway and nivolumab clinical trial evaluation 436).
Primary Endpoint	For nivolumab (240 mg intravenously) and BV (1.8 mg/kg intravenously), ORR(95% CI) was 73.00% (54.00% to 88.00%), with a 37.00% complete remission rate per investigator, and ORR of 70.00% (51.00% to 85.00%), with a 43.00% complete metabolic response rate per independent review.
Other Endpoint	For nivolumab (240 mg intravenously) and BV (1.80 mg/kg intravenously), the 6-month PFS rate was 63.50% (95% CI, 42.50 to 78.60), and the 6-month OS rate was 86.30% (95% CI, 67.50 to 94.60). Median PFS and median OS were not reached.
Experiment 23 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Objective Response Rate (ORR)	81.97% (all treated patients) 83.33% (efficacy-evaluable patients)
Patients Enrolled	Refractory Hodgkin lymphoma (defined as not achieving a CR to frontline therapy or progression within 3 months of CR), or Hodgkin lymphoma that had relapsed (defined as progression 3 months after CR to frontline therapy).
Administration Dosage	Received BV (1.80 mg/kg IV, 30-minute infusion) and Nivo (3.00 mg/kg IV, 60-minute infusion) in 3-week cycles for up to 12 weeks (4 cycles). During the first cycle, BV was administered on day 1 and Nivo on day 8. During cycles 2 to 4, BV and Nivo were administered on day 1, with Nivo given at least 30 minutes after BV.
Related Clinical Trial
NCT Number	NCT02572167	Phase Status	Phase 1
Clinical Description	A phase 1/2 study evaluating brentuximab vedotin in combination with nivolumab in patients with relapsed or refractory Hodgkin lymphoma after failure of frontline therapy.
Primary Endpoint	Response rates and Deauville 5-point score for all treated patients (n = 61) and efficacy-evaluable patients (n = 60) are presented. The CR rate among all treated patients was 61.00% (95% CI,47.00%-73.00%). Among efficacy-evaluable patients,the CR rate was 62.00% (95% CI,48.00%-74.00%).
Other Endpoint	Response rates and Deauville 5-point score for all treated patients (n = 61) and efficacy-evaluable patients (n = 60) are presented. The ORR rate among all treated patients was 81.97% (95% CI, 70.00%-91.00%). Among efficacy-evaluable patients, the ORR rate was 83.33% (95% CI,72.00%-92.00%).
Experiment 24 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Objective Response Rate (ORR)	85.00%
Patients Enrolled	Biopsy-proven primary refractory (ie, not achieving a CR or progression <3 months after CR) or relapsed Hodgkin lymphoma (HL; progression 3 months after CR).
Administration Dosage	Received up to 4 cycles of BV 1.80 mg/kg every 3 weeks IV over 30 minutes followed by Nivo 3.00 mg/kg IV over 60 minutes. In parts 1/2 (staggered dosing), BV was administered on day 1 and Nivo on day 8 of cycle 1, with both agents administered on day 1 during cycles 2 to 4. During part 2, the protocol was amended to mandate prophylactic treatment with steroids (hydrocortisone 100 mg or equivalent) and antihistamines (diphenhydramine 25-50 mg or equivalent) at day 1 of each cycle beginning at cycle 2. Patients in part 3 (same-day dosing) received both BV and Nivo on day 1 of all cycles, based on the interim efficacy and safety results in parts 1 and 2 of this study and encouraging results with same-day dosing of both agents in the Eastern Cooperative Oncology Group and the American College of Radiology Imaging Network (ECOG-ACRIN) study E4412.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02572167	Phase Status	Phase 1
Clinical Description	A phase 1/2 study evaluating brentuximab vedotin in combination with nivolumab in patients with relapsed or refractory Hodgkin lymphoma after failure of frontline therapy.
Primary Endpoint	The objective response rate (ORR; N=91) = 85.00%, with 67.00% achieving a complete response (CR); progression-free survival (PFS) rate at 3 years = 77.00% (95% CI, 65.00% to 86.00%) and 91.00% (95% CI, 79.00% to 96.00%) for patients undergoing ASCT directly after study treatment.
Other Endpoint	OS= 93.00% (95% CI, 85.00% to 97.00%) at 3 years.
Experiment 25 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Objective Response Rate (ORR)	100.00%	Positive CD30 expression (CD30+++/++)
Patients Enrolled	CD30 peripheral T-cell lymphoma.
Administration Dosage	1.8 mg/kg IV once every 3 weeks for 6 cycles.
Related Clinical Trial
NCT Number	NCT01309789	Phase Status	Phase 1
Clinical Description	A phase 1 study of brentuximab vedotin given sequentially and combined with multi-agent chemotherapy for CD30-positive mature T-cell and NK-cell neoplasms.
Primary Endpoint	Objective response rate=100.00%.
Other Endpoint	5-year PFS= 52.00%; OS=80.00%
Experiment 26 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Objective Response Rate (ORR)	73.00% (patients with Hodgkin lymphoma who relapsed after ASCT) 86.00% (patients with sALCL)
Patients Enrolled	Hodgkin lymphoma who had relapsed after autologous stem cell transplant (ASCT); systemic anaplastic large-cell lymphoma (sALCL) who had previously been treated with curative intent.
Administration Dosage	1.80 mg/kg, i.v., once every 21 days; a maximum of 16 cycles.
Experiment 27 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Objective Response Rate (ORR)	58.54%
Patients Enrolled	Relapsed or refractory, histologically confirmed CD30-positive hematologic malignancies with bi-dimensional measurable disease of at least 1.5 cm by radiographic evaluation. Patients with Hodgkin lymphoma had received systemic chemotherapy as induction therapy for advanced-stage disease or salvage therapy after initial radiotherapy for early-stage disease and had previously undergone autologous stem cell transplantation (ASCT) unless they were ineligible for or had declined treatment. Patients with other CD30-positive malignancies had previously failed or were refractory to front-line chemotherapy. Patients who had transformed to systemic anaplastic large cell lymphoma (ALCL) were eligible.    Click to Show/Hide
Administration Dosage	Intravenously on Days 1, 8, and 15, of each 28-day cycle at doses ranging from 0.40 to 1.40 mg/kg.
Experiment 28 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Complete Remission (CR)	35.00%
Patients Enrolled	Histologically confirmed rel/ref de novo or transformed diffuse large B-cell lymphoma (DLBCL) after at least 1 prior therapy, Eastern Cooperative Oncology Group (ECOG) performance status 2, and adequate organ function as defined in supplemental Methods.
Administration Dosage	The treatment cycle was 21 days with intravenous BV administered on day 1 and Len administered on days 1 to 21 for a maximum of 16 cycles, the maximum tolerated dose of the combination was 1.20 mg/kg BV with 20 mg/d Len.
Related Clinical Trial
NCT Number	NCT04404283	Phase Status	Phase 3
Clinical Description	A randomized, double-blind, placebo-controlled, active-comparator, multicenter, phase 3 study of brentuximab vedotin or placebo in combination with lenalidomide and rituximab in subjects with relapsed or refractory diffuse large B-cell lymphoma (DLBCL).
Primary Endpoint	The maximum tolerated dose of the combination was 1.20 mg/kg BV with 20 mg/d lenalidomide.
Other Endpoint	The overall response rate was 57.00% (95% CI, 39.60-72.50), complete response rate, 35.00% (95% CI, 20.70-52.60); median duration of response, 13.10 months; median progression-free survival, 10.20 months (95% CI, 5.50-13.70); and median overall survival, 14.30 months (95% CI, 10.20-35.60).
Experiment 29 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Complete Remission (CR)	61.54%
Patients Enrolled	Previously untreated, histologically confirmed stage III/IV classical Hodgkin lymphoma (cHL).
Administration Dosage	A+AVD (brentuximab vedotin, 1.20 mg/kg of bodyweight, doxorubicin 25 mg/m2 of body surface area, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) or ABVD (doxorubicin 25 mg/m2, bleomycin 10 U/m2, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) intravenously on days 1 and 15 of each 28-day cycle for up to six cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD versus ABVD as frontline therapy in patients with advanced classical hodgkin lymphoma.
Primary Endpoint	For 1.20 mg/kg BV intravenously, the 3-year PFS rates=83.10% (95% CI, 79.90-85.90) in the A+AVD arm.
Other Endpoint	For 1.20 mg/kg BV intravenously, complete resolution(CR)=61.54% of (272/442) in the A+AVD arm.
Experiment 30 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Complete Remission (CR)	71.33%
Patients Enrolled	Previously untreated patients (18 years with an Eastern Cooperative Oncology Group performance status of 2) with stage III or IV classical Hodgkin lymphoma.
Administration Dosage	A+AVD (brentuximab vedotin, 1.20 mg/kg of bodyweight, doxorubicin 25 mg/m2 of body surface area, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) or ABVD (doxorubicin 25 mg/m2, bleomycin 10 U/m2, vinblastine 6 mg/m2, and dacarbazine 375 mg/m2) intravenously on days 1 and 15 of each 28-day cycle for up to six cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD versus ABVD as frontline therapy in patients with advanced classical hodgkin lymphoma.
Primary Endpoint	For 1.20 mg/kg BV intravenously, 5-year PFS rates=82.20% (95% CI 79.00-85.00) with A+AVD.
Other Endpoint	For 1.20 mg/kg BV intravenously, complete resolution(CR)=71.33% of (316/443) of patients with peripheral neuropathy in the A+AVD arm. Peripheral neuropathy occurred in 443 (66.91%) of 662 patients in the A+AVD group.
Experiment 31 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Complete Remission (CR)	12.00%
Patients Enrolled	Part (A) relapsed/refractory CD30-expressing mature T-cell and B-cell non-Hodgkin lymphomas (NHL), including DLBCL; Part (B) brentuximab vedotin plus rituximab in relapsed/refractory CD30-expressing DLBCL; and Part (C) single-agent brentuximab vedotin in relapsed/refractory CD30u DLBCL.
Administration Dosage	1.80 mg/kg was administered IV every 21 days.
Related Clinical Trial
NCT Number	NCT01421667	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin in relapsed or refractory non-hodgkin lymphoma (NHL).
Primary Endpoint	ORR=31.00%, median duration=4.70 months (range 0.50-11.60) for 16 patients enrolled on Part C.
Other Endpoint	Six patients had CR (12.00%) with a median duration of 11.60 months (range,1.40±11.60) and median PFS of 15.60 months (range,3.8±15.6). Overall median PFS was 1.4 months (range, 0.40- 15.60). Median overall survival (OS) was 7.50 months (range, 0.7-18.6).
Experiment 32 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Complete Remission (CR)	35.41%
Patients Enrolled	A clinical and histologically confirmed diagnosis of CD30+ LyP, CD30+ pc-anaplastic large-cell lymphoma (ALCL), or myelofibrosis (MF). Eastern Cooperative Oncology Group performance status of 2 and adequate bone marrow and organ function were required.
Administration Dosage	Intravenously at 1.80 mg/kg every 21 days for a maximum of eight doses.
Related Clinical Trial
NCT Number	NCT01352520	Phase Status	Phase 2
Clinical Description	Phase 2 trial of brentuximab vedotin (SGN-35) at dose of 1.80 mg/kg IV every 3 weeks in patients with CD30-positive lymphoproliferative disorders (cutaneous anaplastic large T-cell lymphoma (ALCL), mycosis fungoides, and extensive lymphomatoid papulosis (LyP).
Primary Endpoint	Os rate=72.92% (95% CI, 60.00% to 86.00%; 35 of 48 patients), CR raate=35.41% (95% CI, 22.00% to 49.00%; 17 of 48 patients). Fifteen (53.57%; 95% CI, 31% to 59%) of 28 patients with MF responded, independent of CD30 expression.
Other Endpoint	In patients with MF/Szary syndrome, the overall response rate was 50.00% (five of 10 patients) in patients with low CD30 expression (< 10%), 58.33% (seven of 12 patients) in patients with medium expression (10% to 50%), and 50.00% (three of six patients) in patients with high expression (50%).
Experiment 33 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Complete Remission (CR)	43.00% (In 56 evaluable patients treated across cohorts)
Patients Enrolled	Patients over 10 years of age with biopsy-proven cHL that had relapsed or was primary refractory (lack of CR or PD within 3months of upfront therapy) after standard initial therapy were eligible.
Administration Dosage	1.80 mg/kg intravenously every 3 weeks for two cycles.
Related Clinical Trial
NCT Number	NCT01393717	Phase Status	Phase 2
Clinical Description	A phase 2 study of brentuximab vedotin as salvage therapy for hodgkin lymphoma prior to autologous hematopoietic stem cell transplantation.
Primary Endpoint	The 2-year PFS among patients in CR at the time of AHCT (n=37) was 71% compared with 54% in patients not in CR (p=0.12). The 2-year PFS in patients who proceeded to AHCT directly after receiving BV alone was 77%.
Other Endpoint	Of 56 evaluable patients treated across cohorts, the overall response rate (ORR) to second-line BV was 75.00% with 43.00% CR.
Experiment 34 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Complete Remission (CR)	58.00%
Patients Enrolled	LyP and were also required to have scarring, more than 10 lesions, or active lesions on the face, hands, or feet.
Administration Dosage	Intravenous brentuximab vedotin 1.80 mg/kg infused over 30 minutes every 21 days.
Related Clinical Trial
NCT Number	NCT01352520	Phase Status	Phase 2
Clinical Description	Phase 2 trial of brentuximab vedotin (SGN-35) at dose of 1.80 mg/kg IV every 3 weeks in patients with CD30-positive lymphoproliferative disorders (cutaneous anaplastic large T-cell lymphoma (ALCL), mycosis fungoides, and extensive lymphomatoid papulosis (LyP).
Primary Endpoint	The overall response rate was 100% and at 4 months was 80% (8 of 10 patients).
Experiment 35 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Complete Remission (CR)	14.70%
Patients Enrolled	Steroid-refractory acute graft-versus-host disease (SR-aGVHD).
Administration Dosage	The study included weekly dosing for 3 weeks followed by maintenance dosing every 3 weeks for an 4 additional doses. A standard 3+3 dose-escalation cohort (0.60 mg/kg, 0.90 mg/kg, and 1.20 mg/kg) was planned to define the maximum tolerated dose (MTD). After treating the first 6 patients, the study was revised to dosing every 2 weeks for 4 doses only for safety purposes, and to enroll cohorts of 5 patients at each dose level (0.60 mg/kg, 0.80 mg/kg, 1.00 mg/kg, and 1.20 mg/kg).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01940796	Phase Status	Phase 1
Clinical Description	Phase 1 trial of brentuximab vedotin for refractory chronic graft-vs.-host disease (GVHD).
Primary Endpoint	The MTD was defined at 0.80 mg/kg with one DLT observed (sepsis).
Other Endpoint	At day 28, the overall response rate was 38.20% with 5 complete responses (CR, 14.70%) and 8 very good partial responses (VGPR, 23.50%).Overall survival was 41.00% (95% CI, 25.00%-57.00%) at 6 months and 38.00% (95% CI, 22.00%-54.00%) at 12 months.
Experiment 36 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Complete Remission (CR)	35.00%
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma (DLBCL); have previously received at least two lines of therapy, including rituximab and an anthracycline; patients had either had a relapse after or were ineligible for autologous transplantation.
Administration Dosage	1.20 mg/kg intravenously (IV) on Day 1 of every 21 day cycle.
Related Clinical Trial
NCT Number	NCT02086604	Phase Status	Phase 1
Clinical Description	A phase 1 trial of brentuximab vedotin in combination with lenalidomide in relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	Most patients required granulocyte colony-stimulating factor support because of neutropenia. The overall response rate was 57.00% (95% CI, 39.60-72.50), complete response rate, 35.00% (95% CI, 20.70-52.60); median duration of response, 13.10 months; median progression-free survival, 10.20 months (95% CI, 5.50-13.70); and median overall survival, 14.30 months (95% CI, 10.20-35.60). Response rates were highest in patients with CD301 DLBCL (73.00%), but they did not differ according to cell of origin (P=5.96).    Click to Show/Hide
Experiment 37 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Complete Remission (CR)	66.67%
Patients Enrolled	Primary refractory Hodgkin Lymphoma or early relapse. Eligibility criteria included age 30 years; no prior Brentuximab vedotin exposure; and relapse <1 year from completion of initial therapy.
Administration Dosage	Each 21-day cycle consisted of intravenous day 1 at 1.40 mg/kg or 1.80 mg/kg.
Related Clinical Trial
NCT Number	NCT01780662	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of brentuximab vedotin (SGN35) in combination with gemcitabine for pediatric and young adult patients with relapsed or refractory Hodgkin lymphoma.
Primary Endpoint	For four of the 13 patients with stable disease or partial response,all target lesions were Deauville score 3 on central review,and would thus be considered CRs by response criteria published after AHOD1221 opened. By these criteria,the complete response rate observed on AHOD1221 was 28 of 42 patients (66.67%; 95% CI, 51.00-80.00%).
Experiment 38 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Complete Remission (CR)	74.00%
Patients Enrolled	First relapse or primary refractory classic Hodgkin lymphoma (CHL) after one prior line of therapy.
Administration Dosage	Days 1 and 8 at either 1.20 or 1.50 mg/kg IV (capped at 150 mg) with standard dosing of ICE on days 13 for two cycles.
Related Clinical Trial
NCT Number	NCT02227199	Phase Status	Phase 1
Clinical Description	A phase 1/2 trial of brentuximab vedotin (BV), ifosfamide (I), carboplatin (C), and etoposide (E) for patients with relapsed or refractory Hodgkin lymphoma (BV-ICE).
Primary Endpoint	Rp2D=BV 1.50 mg/kg IV CR=74.00%.
Other Endpoint	ORR=91.00%.
Experiment 39 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Complete Remission (CR)	86.00%
Patients Enrolled	CD30+ primary mediastinal large B-cell lymphoma (PMBCL), diffuse large B-cell lymphoma (DLBCL), or gray zone lymphoma (GZL). Patients with any stage, measurable disease, and an Eastern Cooperative Oncology Group Performance Status of 3 or less were eligible. The diagnostic biopsy had to demonstrate at least 1% or higher expression of CD30 on the lymphoma B cells by immunohistochemistry and was assessed independently by two pathologists. Patients with active central nervous system involvement and uncontrolled systemic infections were excluded.    Click to Show/Hide
Administration Dosage	Six cycles of BV (1.80 mg/kg, maximum dose of 180 mg) administered with the R-CHOP regimen without vincristine, including: rituximab 375 mg/m2, cyclophosphamide 750 mg/m2, and doxorubicin 50 mg/m2 on day 1 and prednisone 100 mg (or equivalent) daily on days 1 through 5 of each 21-day cycle. For cycle 1, rituximab was split into two doses (100 mg/m2 on day 1 and 275 mg/m2 on day 2) to reduce risks of an infusion reaction to rituximab.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01994850	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of brentuximab vedotin in combination with multi-agent chemotherapy as front-line treatment in patients with CD30 positive primary mediastinal large B-cell, diffuse large B-cell, and grey zone lymphomas.
Primary Endpoint	For Brentuximab vedotin dose of 1.80 mg/kg, the overall response rate was 100.00% (95%CI: 88.00-100.00) with 86.00% (95% CI: 68.00-96.00) of patients achieving complete response at the end of systemic treatment.
Other Endpoint	For Brentuximab vedotin dose of 1.80 mg/kg, the 2-year PFS and overall survival rates were 85.00% (95%CI: 66.00-94.00) and 100.00%, respectively.
Experiment 40 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Complete Remission (CR)	95.45% (brentuximab vedotin + ABVD) 96.00% (brentuximab vedotin + AVD)
Patients Enrolled	Newly diagnosed, treatment-naive, CD30-positive patients with Hodgkin's lymphoma who had histologically confirmed stage IIA bulky disease or stage IIB-IV disease and an Eastern Cooperative Oncology Group performance status of two or less.
Administration Dosage	0.60, 0.90, or 1.20 mg/kg brentuximab vedotin by intravenous infusion every 2 weeks with either ABVD (25 mg/m(2) doxorubicin, 10 units/m(2) bleomycin, 6 mg/m(2) vinblastine, and 375 mg/m(2) dacarbazine) or AVD (ABVD modified regimen without the inclusion of bleomycin) for up to six cycles.
Related Clinical Trial
NCT Number	NCT01060904	Phase Status	Phase 1
Clinical Description	A phase 1 dose-escalation safety study of brentuximab vedotin in combination with multi-agent chemotherapy as frontline therapy in patients with Hodgkin lymphoma.
Primary Endpoint	The MTD of brentuximab vedotin 1.20 mg/kg ; CR of brentuximab vedotin + ABVD = 95.45%(21/22); CR of brentuximab vedotin + AVD = 96.00%(24 /25 ).
Other Endpoint	Maximum tolerated dose was not exceeded at 1.20 mg/kg of brentuximab vedotin combined with either ABVD or AVD.
Experiment 41 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Complete Remission (CR)	60.00% (BV + R therapy)
Patients Enrolled	Had prior solid organ or hematopoietic stem cell transplantation, received immunosuppressive therapy for a nonmalignant condition, and/or had an aggressive EBV+lymphoid malignancy.
Administration Dosage	Induction therapy consisted of R 375 mg/m2 given on days 1, 8, 15, 22, and BV 1.20 mg/kg given on days 1, 8, 15, followed by restaging as assessed by CT imaging. MT consisted of BV 1.8 mg/kg every 3 weeks and R 375 mg/m2 every 6 weeks for up to one year of total therapy.
Experiment 42 Reporting the Activity Date of This ADC					[66]
Patients Enrolled	Previously untreated Hodgkins lymphoma of stage IIB with bulk tumor or stage IIIB, IVA, or IVB.
Administration Dosage	Brentuximab vedotin (at a dose of 1.80 mg per kilogram) plus doxorubicin, vincristine, etoposide, prednisone, and cyclophosphamide or the standard bleomycin-containing chemotherapy regimen was administered every 21 days.
Related Clinical Trial
NCT Number	NCT02166463	Phase Status	Phase 3
Clinical Description	A randomized phase 3 study of brentuximab vedotin (SGN-35) for newly diagnosed high-risk classical hodgkin lymphoma (cHL) in children and young adults.
Primary Endpoint	At a median follow-up of 42.10 months (range, 0.10 to 80.90), the 3-year event-free survival was 92.10% (95% confidence interval [CI],88.40 to 94.70) in the brentuximab vedotin group.
Other Endpoint	Overall survival at 3 years was 99.30% (95% CI,97.30 to 99.80) in the brentuximab vedotin group.
Experiment 43 Reporting the Activity Date of This ADC					[67]
Patients Enrolled	III or IV Hodgkins lymphoma.
Administration Dosage	1.20 mg of brentuximab vedotin per kilogram of body weight, 25 mg of doxorubicin per square meter of body-surface area, 6 mg of vinblastine per square meter, and 375 mg of dacarbazine per square meter; intravenously on days 1 and 15 of each 28-day cycle for up to six cycles.
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD Versus ABVD as frontline therapy in patients with advanced classical hodgkin lymphoma.
Primary Endpoint	The analysis of overall survival significantly favored A+AVD over ABVD (95% CI,0.40-0.88).The 6-year overall survival estimates were 93.90% (95% CI,91.60 to 95.50) in the A+AVD group and 89.40% (95% CI,86.60 to 91.70) in the ABVD group.
Other Endpoint	The median follow-up in the overall survival analysis was 73.00 months (95% CI,72.30 to 73.60; range,0.0 to 100.6). A total of 39 deaths occurred in the A+AVD group and 64 in the ABVD group.
Experiment 44 Reporting the Activity Date of This ADC					[68]
Patients Enrolled	Advanced classic Hodgkins lymphoma (Ann Arbor stage III or IV, as determined on a 4-point scale, with higher stages indicating more widespread disease),17 according to the World Health Organization classification system. Patients who had not been previously treated with systemic chemotherapy or radiotherapy were eligible. Patients were required to have an Eastern Cooperative Oncology Group performance status of 0, 1, or 2 (on a scale of 0 to 5, with higher scores indicating greater disability).    Click to Show/Hide
Administration Dosage	A+AVD (1.20 mg of brentuximab vedotin per kilogram of body weight, 25 mg of doxorubicin per square meter of body-surface area, 6 mg of vinblastine per square meter, and 375 mg of dacarbazine per square meter) or ABVD (25 mg of doxorubicin per square meter, 10 units of bleomycin per square meter, 6 mg of vinblastine per square meter, and 375 mg of dacarbazine per square meter) intravenously on days 1 and 15 of each 28-day cycle for up to 6 cycles.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01712490	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of A+AVD versus ABVD as frontline therapy in patients with advanced classical Hodgkin lymphoma.
Primary Endpoint	After a median follow-up of 24.90 months (range, 0 to 49.30), the rate of the primary end point of independently determined modified progression-free survival was significantly higher in the A+AVD group than in the ABVD group (2-year modified progression-free survival rate, 82.10% [95% confidence interval {CI}, 78.70 to 85.00] vs. 77.20% [95% CI, 73.70 to 80.40]; hazard ratio for progression, death, or modified progression, 0.77 [95% CI, 0.60 to 0.98]; P = 0.03), corresponding to a 23.00% risk reduction.    Click to Show/Hide
Other Endpoint	The interim 2-year overall survival rate for the A+AVD group was 96.60% (95% CI,94.80 to 97.70) and that for the ABVD group was 94.90% (95% CI,92.90 to 96.40),which corresponded to a reduction in the risk of death of 28.00% in favor of the A+AVD regimen (hazard ratio,0.72; 95% CI,0.44 to 1.17; P = 0.19).
Experiment 45 Reporting the Activity Date of This ADC					[69]
Patients Enrolled	CD30-positive mycosis fungoides or primary cutaneous anaplastic large-cell lymphoma who had been previously treated.
Administration Dosage	Interactive voice and web response system to receive intravenous brentuximab vedotin 1.80 mg/kg once every 3 weeks, for up to 16 3-week cycles.
Related Clinical Trial
NCT Number	NCT01578499	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of brentuximab vedotin (SGN-35) versus physician's choice (methotrexate or bexarotene) in patients with CD30-positive cutaneous T-cell lymphoma.
Primary Endpoint	At a median follow-up of 22.90 months (95% CI 18.40-26.10), the proportion of patients achieving an objective global response lasting at least 4 months was 56.25% (36 of 64 patients) with brentuximab vedotin versus 12.50% (8/64) with physicians choice, resulting in a between-group difference of 43.80% (95% CI 29.10-58.40).
Other Endpoint	Median progression-free survival per EMA criteria was 16.70 months in the brentuximab vedotin group versus 3.50 months in the physicians choice group (HR 0.270, 95% CI 0.169-0.430).
Experiment 46 Reporting the Activity Date of This ADC					[70]
Patients Enrolled	Patients aged 18 years with previously treated CD30-expressing myelofibrosis (MF) or classic anaplastic large-cell lymphoma (after at least 1 prior systemic therapy or prior radiotherapy) were enrolled; CD30 positivity was defined as 10% of target lymphoid cells exhibiting a membrane, cytoplasmic, and/or Golgi staining pattern for CD30. An Eastern Cooperative Oncology Group performance status of 0 to 2 was required.    Click to Show/Hide
Administration Dosage	Brentuximab vedotin (1.80 mg/kg IV every 3 weeks, for up to 16 cycles) or physicians choice (methotrexate, 5-50 mg orally once weekly or bexarotene 300 mg/m2 [target dose] orally once daily, for up to 48 weeks).
Related Clinical Trial
NCT Number	NCT01578499	Phase Status	Phase 3
Clinical Description	A previously treated, recurrent or metastatic cervical cancer (SGN-35) versus physician's choice (methotrexate or bexarotene) in patients with CD30-positive cutaneous T-cell lymphoma.
Primary Endpoint	For 1.80 mg/kg BV intravenously, objective responses lasting 4 months (ORR4) was 54.70%; the ORR per IRF was 65.60%.
Other Endpoint	For 1.80 mg/kg BV intravenously, the CR rate was 17.20%; median PFS 16.70 (95% CI, 0.25-0.58); 3-year estimates of OS was 64.40% (95% CI, 0.42-1.32); time to next treatment (TTNT) was 14.20 (95% CI, 0.17-0.42).
Experiment 47 Reporting the Activity Date of This ADC					[73]
Patients Enrolled	High-risk relapsed or refractory classic Hodgkin lymphoma, had an ECOG performance status of 0-2, and had adequate organ and bone marrow function.
Administration Dosage	Enrolled patients received brentuximab vedotin (1.8 mg/kg) intravenously starting 30-60 days after autologous HSCT on day 1 of each 21-day cycle for up to 8 cycles.
Related Clinical Trial
NCT Number	NCT03057795	Phase Status	Phase 2
Clinical Description	A phase 2 study of nivolumab and brentuximab vedotin consolidation after autologous stem cell transplantation in patients with high-risk classical hodgkin lymphoma.
Primary Endpoint	The 18-month progression-free survival in all 59 patients was 94% (95% CI 84-98).
Other Endpoint	The 24-month overall survival was 98.00% (95% CI 88.00-100.00). The 24-month progression-free survival according to the number of risk factors was 94.00% (95% CI 67.00-99.00) in patients with one risk factor (n=21),96.00% (73.00-99.00) in patients with two risk factors (n=24), and 85.00% (51.00-96.00) in patients with three or more risk factors (n=14). The 24-month cumulative incidence of relapse and progression was 5.70% (95% CI 1.50-14.00); the 24-month cumulative incidence of non-relapse mortality was 1.80% (0.14-8.40).    Click to Show/Hide
Experiment 48 Reporting the Activity Date of This ADC					[74]
Patients Enrolled	Histologically proven anaplastic lymphoma kinase (ALK)+ anaplastic large-cell lymphoma (ALCL) and were younger than 22 years of age at diagnosis.
Administration Dosage	Brentuximab vedotin was administered on day 1 of each of the 6 cycles for a total of 6 doses. The starting dose of brentuximab vedotin was 1.80 mg/kg (maximum dose, 180 mg) given IV over 30 minutes on day 1 of each cycle prior to all other chemotherapy. Dose reductions to 1.20 mg/kg (maximum dose, 120 mg), followed by 0.80 mg/kg (maximum dose, 80 mg), were mandated for certain toxicities.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01979536	Phase Status	Phase 2
Clinical Description	A randomized phase 2 trial of brentuximab vedotin (SGN35, NSC# 749710), or crizotinib (NSC#749005, commercially labeled) in combination with chemotherapy for newly diagnosed patients with anaplastic large cell lymphoma (ALCL).
Primary Endpoint	For 1.80 mg/kg BV intravenously, the complete response rate (complete response + complete response, unconfirmed) was 62.12% for patients who underwent evaluation after cycle 2 (41/66 patients) and 96.88% after cycle 6 (62/64 patients).
Other Endpoint	For 1.80 mg/kg BV intravenously, The 2-year event-free survival (EFS)=79.10% (95%CI, 67.20-87.10). The 2-year overall survival (OS)=97.00% (95% CI, 88.10-99.20).
Experiment 49 Reporting the Activity Date of This ADC					[75]
Patients Enrolled	Metastatic non-seminomatous germ cell tumor (GCT) with the exception of pure teratoma who progressed after first-line cisplatin-based chemotherapy and after at least one salvage regimen.
Administration Dosage	1.80 mg/kg IV every 3 weeks until disease progression or intolerable toxicities.
Related Clinical Trial
NCT Number	NCT01461538	Phase Status	Phase 2
Clinical Description	A phase 2, open-label study of brentuximab vedotin in patients with CD30-positive nonlymphomatous malignancies.
Primary Endpoint	For 1.80 mg/kg BV intravenously, Median PFS in the CD30 positive cohort was 1.20 months (95% CI: 0.90-2.10) and in the CD30 negative cohort was 1.40 months (95% CI: 0.00-2.10). Median OS in the CD30 positive cohort was 2.50 months (95% CI: 1.10-12.90) and in the CD30 negative cohort was 5.90 months (95% CI: 1.60-8.20).
Experiment 50 Reporting the Activity Date of This ADC					[76]
Patients Enrolled	46 patients with classic Hodgkin lymphoma, unsuitable for standard chemotherapy because of a cardiac ejection fraction of less than 50%, pulmonary diffusion capacity of less than 80%, or a creatinine clearance of 30 mL/min or more but less than 60 mL/minrequired to have an Eastern Cooperative Oncology Group (ECOG) performance status of 0-2.
Administration Dosage	Brentuximab vedotin (1.8 mg/kg, dose cap at 180 mg) and nivolumab (3 mg/kg) intravenously every 21 days for 8 cycles.
Related Clinical Trial
NCT Number	NCT02758717	Phase Status	Phase 2
Clinical Description	Phase II, multi-center trial of nivolumab and brentuximab vedotin in patients with untreated Hodgkin lymphoma over the age of 60 years or unable to receive standard adriamycin, bleomycin, vinblastine, and dacarbazine (ABVD) chemotherapy.
Primary Endpoint	The overall response, defined as a partial metabolic response or complete metabolic response at the end of 8 cycles of treatment
Other Endpoint	The complete metabolic response rate, safety and tolerability of the regimen in this population, duration of response, progression-free survival, and overall survival.
Experiment 51 Reporting the Activity Date of This ADC					[77]
Related Clinical Trial
NCT Number	NCT02686346	Phase Status	Phase 1/2
Clinical Description	Phase 1/2 feasibility study of brentuximab vedotin in refractory/relapsed hodgkin lymphoma patients who are treated by chemotherapy (ICE) in second line and eligible for autologous transplantation.

Experiment 1 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0.00% (Day 40)	Positive CD30 expression (CD30+++/++)
Method Description	3 mg conjugate/kg/inj.
In Vivo Model	L2987 cell line xenograft model
In Vitro Model	Lung adenocarcinoma	L2987 cells		CVCL_H586
Experiment 2 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.40% (Day 35)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	L-540 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 31.50% (Day 35)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 4 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.70% (Day 53)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 5 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.40% (Day 35)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 6 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.80% (Day 35)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	L-540 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 7 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.70% (Day 53)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination Brentuximab Vedotin with TGR-1202 (PI3K- inhibitor) against cancer cell growth was evaluated in the HL xenograft model. Six- to eight-week-old NOD/SCID mice (20 to 25 g) were xenografted with L-540 (2.5x106 cells/mouse) and KM-H2 (2.0x106 cells/mouse) cells by inoculation into the left flank. When the tumor volume reached approximately 100 mg, the mice were randomly assigned to receive TGR-1202 (150 mg/kg/5 day/3 wks, PO) and/or BV (0.5 mg/kg/q4d/2 weeks, IP).    Click to Show/Hide
In Vivo Model	KM-H2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 8 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.80% (Day 56)	Positive CD30 expression (CD30+++/++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. Mice of the ruxolitinib group received ruxolitinib at a dose of 50 mg/kg per day by s.c. inserted osmotic minipumps for 2 wk. Mice of the BV group received BV at 4 mg/kg by i.v. injection every 4 d for three injections. Mice of the combination group received a combination of ruxolitinb with BV at the same doses and dosing schedules as those in the ruxolitinib and BV groups.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 9 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.30% (Day 21)	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 10 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.00% (Day 21)	Moderate CD30 expression (CD30++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 11 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.70% (Day 21)	Negative CD30 expression (CD30-)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 12 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.83% (Day 30)	Positive CD30 expression (CD30+++/++)
Method Description	1 mg conjugate/kg/inj.
In Vivo Model	Karpas 299 ALCL cell line xenograft model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 13 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.20% (Day 15)	Positive CD30 expression (CD30+++/++)
Method Description	0.5 mg/kg/in.
In Vivo Model	Karpas 299 ALCL cell line xenograft model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 14 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80% (Day 56)	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. Mice of the ruxolitinib group received ruxolitinib at a dose of 50 mg/kg per day by s.c. inserted osmotic minipumps for 2 wk. Mice of the BV group received BV at 4 mg/kg by i.v. injection every 4 d for three injections. Mice of the combination group received a combination of ruxolitinb with BV at the same doses and dosing schedules as those in the ruxolitinib and BV groups.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 15 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.90% (Day 21)	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of all possible combination regimens of ruxolitinib, Navitoclax, and BV against cancer cell growth was evaluated in the HDLM-2 xenograft mouse model of human HL. The xenograft tumor model of human HL HDLM-2 was established by s.c. injection of 2x107 HDLM-2 cells into the right flank of female, 8-wk-old, NOD/SCID mice.    Click to Show/Hide
In Vivo Model	HDLM-2 cell line xenograft model
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 16 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Tumor Growth Delay (TGD)	40 Day (Median)	High CD30 expression (CD30+++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 300 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 17 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Tumor Growth Delay (TGD)	61 Day (Median)	High CD30 expression (CD30+++/++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 300 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 18 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Tumor Growth Delay (TGD)	63 Day (Median)	High CD30 expression (CD30+++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 100 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 19 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Tumor Growth Delay (TGD)	> 80 Day (Median)	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	SCID mice were implanted with L540cy HL cells in the right flank. Groups of mice (9-10/group) were untreated or received SGN-35 (1 mg/kg, q4dx3, i.p.) and/or ABVD [Adriamycin (0.75 mg/kg, q4dx3, i.v.), Bleomycin (6u/kg, q4dx3, i.p.), Vinblastine (0.01 mg/kg, q4dx3, i.p.) and Dacarbazine (15 mg/kg, q3dx4, i.p.)] when tumour size averaged approximately 100 mm3.    Click to Show/Hide
In Vivo Model	L540cy cell line xenograft model
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 20 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.50 ng/mL
Method Description	The inhibitory activity of cAC10 vcMMAE against cancer cell growth was compared with other anti-CD30 mAbs against the growth of a variety of HD and ALCL cell lines in vitro. For localized, subcutaneous disease models of ALCL and HD,5x106 Karpas 299 or 2x107 L540cy cells, respectively, were implanted into the right flanks of C.B.-17/IcrHsd-SCID mice (Harlan, Indianapolis, IN).Therapy with cAC10-vcMMAE or controls was initiated when the tumor size in each group of 5 animals averaged approximately 100 mm3.Treatment consisted of intravenous injections every fourth day for 4 injections (q4d x 4).    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.90 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.70 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.20 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.50 pM
Method Description	The inhibitory activity of Brentuximab vedotin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 5 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.50 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 6 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	CESS cells		CVCL_0209
Experiment 7 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	63.00 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90.00 ng/mL
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Hodgkin lymphoma	KM-H2 cells		CVCL_1330
Experiment 9 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	219.50 ng/mL
Method Description	The inhibitory activity of Brentuximab Vedotin against cancer cell growth was evaluated in CD30positive GCT27 cell line in vitro. The cells were treated with 250 ng/mL ADC for 96 hours.
In Vitro Model	Testicular teratoma	GCT 27 cells		CVCL_A344
Experiment 10 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1013.00 ng/mL
Method Description	The inhibitory activity of Brentuximab Vedotin against cancer cell growth was evaluated in CD30negative JAR cell line in vitro. The cells were treated with 1000 ng/mL ADC for 96 hours.
In Vitro Model	Gestational choriocarcinoma	JAR cells		CVCL_0360
Experiment 11 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1400.80 ng/mL
Method Description	The inhibitory activity of Brentuximab Vedotin against cancer cell growth was evaluated in moderate expression NCCIT cell line in vitro. The cells were treated with 500 ng/mL ADC for 96 hours.
In Vitro Model	Testicular embryonal carcinoma	NCC-IT cells		CVCL_1451
Experiment 12 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3300.00 ng/mL 1.30 ng/mL 9.90 ng/mL
Method Description	The antitumor activity of SGN-35 was prepared with 14C-labeled MMAE. Intracellular ADC activation on CD30+ and negative cell lines was determined using a combination of radiometric and liquid chromatograhpy/mass spectrometry-based assays. The bystander activity of SGN-35 was determined using mixed tumor cell cultures consisting of CD30+ and CD30 lines.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
	Diffuse large B-cell lymphoma	WSU-NHL cells		CVCL_1793
	Hodgkin's disease	L540cy cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Partial Response (PR)	40.00%	Moderate Tissue factor expression (TF++; IHC H-score=155)
Patients Enrolled	Ovary Cancer; Cervix Cancer; Endometrium Cancer; Bladder Cancer; Prostate Cancer; Esophagus Cancer; Lung Cancer, Nonsmall Cell; Squamous Cell Carcinoma of the Head and Neck.
Administration Dosage	Once every 3 weeks intravenous (IV).
Related Clinical Trial
NCT Number	NCT03245736	Phase Status	Phase 2
Clinical Description	A multi-center, open-label trial investigating the efficacy and safety of continued treatment with tisotumab vedotin in patients with solid tumors known to express tissue factor.
Primary Endpoint	Number of participants who experienced a treatment emergent adverse event (TEAE): 5/5 Participants (100%).
Other Endpoint	Partial Response Rate=2/5 (40.00%), Stable Disease Rate=2/5(40.00%), Progressive Disease Rate=1/5 (20.00%), Increased Cancer Antigen (CA 125) Levels Rate=1/2 (50.00%).
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Objective Response Rate (ORR)	24.00%	High Tissue factor expression (TF+++; IHC H-score=250)
Patients Enrolled	Recurrent or metastatic squamous cell, adenocarcinoma, or adenosquamous cervical cancer; disease progression on or after doublet chemotherapy with bevacizumab (if eligible by local standards); who had received two or fewer previous systemic regimens for recurrent or metastatic disease; had measurable disease based on Response Evaluation Criteria in Solid Tumors (RECIST; version 11); and had an Eastern Cooperative Oncology Group performance status of 0 or 1.    Click to Show/Hide
Administration Dosage	20 mg/kg (up to a maximum of 200 mg) intravenously once every 3 weeks.
Related Clinical Trial
NCT Number	NCT03438396	Phase Status	Phase 2
Clinical Description	A Single arm, multicenter, international trial of tisotumab vedotin (HuMax-TF-ADC) in previously treated, recurrent or metastatic cervical cancer.
Primary Endpoint	Objective response rate=24.00% (95% CI 16.00%-33.00%), comprising 7 (7.00%) complete responses and 17 (17.00%) partial responses, Disease Control Rate (DCR)=72.00%.
Other Endpoint	Median duration of response=8.30 months, 62.00% (95% CI 3.70-8.00) of patients > 6months,median progression-free survival = 4.20 months (95% Cl 3.00-4.40), median overall survival = 12.10 months (95% Cl, 9.60-13.90).
Experiment 3 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Objective Response Rate (ORR)	38.24% (second- or third-line group)	Low Tissue factor expression (TF+; <7,000 TF molecules/cell)
Patients Enrolled	Recurrent/metastatic cervical cancer (r/mCC).
Administration Dosage	20 mg/kg + pembro 200 mg IV Q3W.
Related Clinical Trial
NCT Number	NCT03786081	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 open-label trial of tisotumab vedotin (HuMax-TF-ADC) monotherapy and in combination with other agents in subjects with recurrent or stage IVB cervical cancer.
Primary Endpoint	In the second- or third-line group,objective response rate=38.24% (95% Cl 22.00-56.00), comprising 2 (5.88%) complete responses and 11 (32.35%) partial responses.
Other Endpoint	In the second- or third-line group,median duration of response was 13.80 months, median progression-free survival was 5.60 months.
Experiment 4 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Objective Response Rate (ORR)	54.55% (first-line treatment group)	High Tissue factor expression (TF+++; >300,000 TF molecules/cell)
Patients Enrolled	Recurrent/metastatic cervical cancer (r/mCC).
Administration Dosage	20 mg/kg + carbo AUC 5 IV every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT03786081	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 open-label trial of tisotumab vedotin (HuMax-TF-ADC) monotherapy and in combination with other agents in subjects with recurrent or stage IVB cervical cancer.
Primary Endpoint	In the first-line treatment group, objective response rate= 54.55%, comprising 4 (12.12%) complete responses and 14 (42.42%) partial responses.
Other Endpoint	In the first-line treatment group, median duration of response=83 months,median progression-free survival was 95 months.
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Objective Response Rate (ORR)	15.65% (all patients) 26.67% (Bladder cancer) 26.47% (Cervical cancer) 7.14% (Endometrial cancer) 13.33% (Oesophageal cancer) 13.33% (NSCLC) 13.89% (Ovarian cancer)	Low Tissue factor expression (TF+; <15,000 TF molecules/cell)
Patients Enrolled	Relapsed, advanced, or metastatic cancer of the ovary, cervix, endometrium, bladder, prostate, oesophagus, squamous cell carcinoma of the head and neck or non-small-cell lung cancer; an Eastern Cooperative Oncology Group performance status of 0-1; and had relapsed after or were not eligible to receive the available standard of care.
Administration Dosage	0.3 and 2.2 mg/kg intravenously once every 3 weeks in a traditional 3+3 design.
Related Clinical Trial
NCT Number	NCT02001623	Phase Status	Phase 1/2
Clinical Description	First-in-human, dose-escalating safety study of tissue factor specific antibody drug conjugate tisotumab vedotin (HuMax TF ADC) in patients with locally advanced and/or metastatic solid tumors known to express tissue factor.
Primary Endpoint	OrR of all patients=15.65% (23/147, 95% Cl 10.20-22.00), ORR of Bladder cancer=26.67% (4/15, 95% Cl 7.80-55.10), ORR of Cervical cancer=26.47% (9/34, 95% Cl 12.90-44.40), ORR of Endometrial cancer=7.14% (1/14, 95% Cl 0.20-33.90), ORR of Oesophageal cancer=13.33% (2/15, 95% Cl 1.70-40.50), ORR of NSCLC=13.33% (2/15, 95% Cl 1.70-40.50), ORR of Ovarian cancer=13.89% (5/36, 95% Cl 4.70-29.50).    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Objective Response Rate (ORR)	24.00%	High Tissue factor expression (TF+++; IHC H-score=250)
Patients Enrolled	Cervical cancer.
Administration Dosage	20 mg/kg every 3 weeks.
Related Clinical Trial
NCT Number	NCT02001623	Phase Status	Phase 1/2
Clinical Description	First-in-human, dose-escalating safety study of tissue factor specific antibody drug conjugate tisotumab vedotin (HuMax TF ADC) in patients with locally advanced and/or metastatic solid tumors known to express tissue factor.
Primary Endpoint	Objective response rate=24.00% (95% Cl 13.00%-37.00%).
Other Endpoint	Median duration of response was 4.20 months (range: 1.00-9.70 months), comprising four patients responding for > 8 months Six-month progression-free survival was 29.00% (95% CI 17.00-43.00).
Experiment 7 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Objective Response Rate (ORR)	29.41%	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Patients Enrolled	Recurrent/metastatic cervical cancer (r/mCC).
Administration Dosage	15 or 20 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number	NCT03913741	Phase Status	Phase 1/2
Clinical Description	Open label phase 1/2 trial of tisotumab vedotin in japanese subjects with advanced solid malignancies.
Primary Endpoint	OrR (CR+PR)=29.41% (95% Cl, 10.30-56.00), Disease Control Rate (DCR)=70.60% (95% Cl 44.00-89.70), CR=0/17 (0%), PR=5/17 (29.41%), SD=7/17 (41.17%), PD=2/17 (11.76%).
Other Endpoint	Median TTR=12 months (range, 11-27 months), median DOR=7.10 months (range, 3.10 months to not reached), median OS=11.4 months (95% Cl 6.2 -not reached) Kaplan-Meier estimates showed that the percentages of patients with an OS 6 months and 12 months were 81.60% (95% CI, 53.00-93.70) and 25.70% (95% CI, 16.00-63.90), respectively.
Experiment 8 Reporting the Activity Date of This ADC					[4]
Related Clinical Trial
NCT Number	NCT04697628	Phase Status	Phase 3
Clinical Description	A randomized, open-label, phase 3 trial of tisotumab vedotin vs investigator's choice chemotherapy in second- or third-line recurrent or metastatic cervical cancer.
Experiment 9 Reporting the Activity Date of This ADC					[4]
Related Clinical Trial
NCT Number	NCT03657043	Phase Status	Phase 2
Clinical Description	Open label phase 2 study of tisotumab vedotin for patients with platinum-resistant ovarian cancer with a safety run-in of a dose-dense regimen.
Experiment 10 Reporting the Activity Date of This ADC					[4]
Related Clinical Trial
NCT Number	NCT03485209	Phase Status	Phase 2
Clinical Description	Open label phase 2 study of tisotumab vedotin for locally advanced or metastatic disease in solid tumors.
Experiment 11 Reporting the Activity Date of This ADC					[4]
Related Clinical Trial
NCT Number	NCT02552121	Phase Status	Phase 1/2
Clinical Description	Dose-escalating and cohort expansion safety trial of tissue factor specific antibody drug conjugate tisotumab vedotin (HuMax-TF-ADC) in patients with locally advanced and/or metastatic solid tumors known to express tissue factor.

Experiment 1 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	72.00% (Day 46)	High Tissue factor expression (TF+++; >300,000 TF molecules/cell)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 190 mm3 The model dosed weekly at 25 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) ovarian carcinomamodel
Experiment 2 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 60)	Low Tissue factor expression (TF+; <15,000 TF molecules/cell)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 210 mm3 The model dosed weekly at 5 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived head and neck carcinoma xenograft (PDX) model
Experiment 3 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 46)	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 140 mm3 The model dosed weekly at 4 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived gastric adenocarcinoma xenograft (PDX) model

Experiment 1 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	71.40% (Day 20)	High Tissue factor expression (TF+++; >300,000 TF molecules/cell)
Method Description	Cell line-derived xenograft models were established in female SCID mice by subcutaneous injection of 5x106 (A431) tumor cells, and treatment with 3 mg/kg TF-ADCs (four injections in 2 weeks) was initiated at day 11 after tumor inoculationDetermined tumor volume after the experiment.
In Vivo Model	A431 cell line xenograft model
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	76.60% (Day 20)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft models were established in female SCID mice by subcutaneous injection of 05x106 (HCT-116) tumor cells, and treatment with 3 mg/kg TF-ADCs (four injections in 2 weeks) was initiated at day 7 after tumor inoculationDetermined tumor volume after the experiment.
In Vivo Model	HCT-116 cell line xenograft model
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 59)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 5 mg/kg for 3 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 20)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft models were established in female SCID mice by subcutaneous injection of 2-10 x106 (HPAF-II) tumor cells, and treatment with 3 mg/kg TF-ADCs (four injections in 2 weeks) was initiated at day 13 after tumor inoculationDetermined tumor volume after the experiment.
In Vivo Model	HPAF-II cell line xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (Tisotumab Vedotin-tftv) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Effective Concentration (EC50)	411.00 ng/mL
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 6 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 ug/mL
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 7 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 mg/mL
Method Description	Cytotoxicity assay in vitroCells were seeded in 96-well plates (2,500-5,000 cells/well) and incubated for 6 hours (37°C), before adding ADCs After 3 to 5 days (37°C), the viability of the culture was assessed Staurosporine ( 10 ug/mL) was used a positive control (100% cell death) and untreated cells were used as a negative control.
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	24.80%	High HER2 expression (HER2+++; IHC 3+)
Patients Enrolled	Locally advanced or metastatic gastric cancer with HER2-overexpression.
Administration Dosage	2.50 mg/kg IV every 2 weeks.
Related Clinical Trial
NCT Number	NCT04714190	Phase Status	Phase 3
Clinical Description	Randomized, controlled, multicenter phase 1/2 clinical study evaluating the efficacy and safety of RC48-ADC for the treatment of locally advanced or metastatic gastric cancer with HER2-overexpression.
Primary Endpoint	The ORR was 24.80% (95% confidence interval [CI]: 17.50%-33.30%).
Other Endpoint	The median PFS and OS were 4.10 months (95% CI: 3.70-4.90 months) and 7.90 months (95% CI: 6.70-9.90 months), respectively. The most frequently reported adverse events were decreased white blood cell count (53.60%), asthenia (53.60%), hair loss (53.60%), decreased neutrophil count (52.00%), anemia (49.60%), and increased aspartate aminotransferase level (43.20%). Serious adverse events (SAEs) occurred in 45 (36.00%) patients, and RC48-related SAEs were mainly decreased neutrophil count (3.20%). Seven patients had adverse events that led to death were not RC48-related.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	24.80%	High HER2 expression (HER2+++; IHC 3+)
Patients Enrolled	HER2overexpressing (IHC 2+ or 3+), locally advanced or metastatic gastric or gastroesophageal junction cancer who were under at least secondline therapy.
Administration Dosage	2.50 mg/kg alone by intravenous infusion during 30-90 min (60 min is recommended) every two weeks.
Related Clinical Trial
NCT Number	NCT03556345	Phase Status	Phase 2
Clinical Description	A multicenter, open label single arm, phase 2 study to evaluate the effect and safety of recombinant humanized anti-HER2 monoclonal antibody-mmae conjugate for injection in HER2 overexpressing local advanced or metastatic gastric cancer.
Primary Endpoint	The ORR was 24.80% (95% confidence interval [CI]: 17.50%-33.30%).
Experiment 3 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Objective Response Rate (ORR)	21.05% (all) 35.71% (HER2 IHC2+/FISH-) 20.00% (IHC2+/FISH+) 13.64% (IHC3+) 15.00% (in patients who were pretreated with HER2-targeted drugs)
Patients Enrolled	Patients with incurable, locally advanced or metastatic solid cancers were eligible for inclusion if their tumors showed HER2 protein overexpression by IHC (3+or 2+), regardless of whether FISH was positive or negative.
Administration Dosage	0.10 mg/kg, 0.50 mg/kg, 1.00 mg/kg, 1.50 mg/kg, 2.00 mg/kg, 2.50 mg/kg, 3.00 mg/kg, 3.50 mg/kg, and 4.00 mg/kg; Q3W; dose expansion proceeded at the dose of 2.00 mg/kg Q2W.
Related Clinical Trial
NCT Number	NCT02881190	Phase Status	Phase 1
Clinical Description	A tolerance, safety and pharmacokinetic ascending dose phase 1 study of RC48-ADC administered intravenously to subjects with HER2-positive malignant in advanced malignant solid tumors.
Primary Endpoint	The MTD was unavailable due to termination of 3.0 mg/kg cohort; 2.5 mg/kg Q2W was declared the RP2D.
Other Endpoint	ORR and DCR were 21.05% (12/57) and 49.12% (28/57). Notably, patients who were HER2 IHC2+/FISH- responded similarly to those who were IHC2+/FISH+and IHC3+, with ORRs of 35.71% (5/14), 20.00% (2/10), and 13.64% (3/22), respectively. In patients who were pretreated with HER2-targeted drugs, RC48 also showed promising efcacy, with ORR of 15.00% (3/20) and DCR of 45.00% (9/20).    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Objective Response Rate (ORR)	51.20%
Patients Enrolled	Advanced or metastatic urothelial cancer.
Related Clinical Trial
NCT Number	NCT04264936	Phase Status	Phase 1
Clinical Description	A open-label, single-arm, phase 1b/2 study of RC48-ADC and JS001 to evaluate the safety and pharmacokinetics of subjects with locally advanced or metastatic urothelial cancer.
Primary Endpoint	The overall confirmed ORR as assessed by the BIRC was 51.20% (95% CI: 35.50%, 66.70%).
Other Endpoint	For RC48-ADC at 2.00 mg/kg, The median PFS and OS were 6.90 months (95% CI: 5.60, 8.90) and 13.90 months (95% CI: 9.10, NE), respectively.
Experiment 5 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Objective Response Rate (ORR)	80.00% (1L previously untreated mUC pts) 75.00% (pts with liver mets) 100.00% (pts with HER2% (3+)) 77.80% (HER2% (2+)) 66.70% (HER2% (1+)) 50.00% (HER2% (0)) 97.10% (in pts with PD-L1 CPS1) 50.00% (in CPS < 1)
Patients Enrolled	HER2-positive and even negative patients (pts) with metastatic urothelial carcinoma (mUC).
Administration Dosage	1.50 or 2.00 mg/kg RC48-ADC + 3 mg/kg toripalimab with the traditional 3+3 escalation design. In the expansion cohort, patients received the recommended dose of RC48-ADC + toripalimab every 2 weeks. The primary endpoints were safety/tolerability and recommended RC48-ADC dose.
Related Clinical Trial
NCT Number	NCT04264936	Phase Status	Phase 1
Clinical Description	A open-label, single-arm, phase 1b/2 study of RC48-ADC and JS001 to evaluate the safety and pharmacokinetics of subjects with locally advanced or metastatic urothelial cancer.
Primary Endpoint	At data cutoff, confirmed investigator-assessed ORR=75.00% (95%CI: 50.90-91.30), including 15.00% CRs; DCR=95.00% (95%CI: 75.10-99.90).
Other Endpoint	The ORR for 1L previously untreated mUC pts was 80.00%. The ORR for pts with liver mets was 75.00%. The ORR was 100.00% for pts with HER2 (3+), 77.80% for HER2 (2+), 66.70% for HER2 (1+), and 50.00% for HER2 (0) respectively. The ORR was 97.10% in pts with PD-L1 CPS1 and 50.00% in CPS < 1.

Experiment 1 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.20% (Day 22)	Moderate HER2 expression (HER2++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model6)
Experiment 2 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.50% (Day 22)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model8)
Experiment 3 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.80% (Day 22)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model9)
Experiment 4 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.80% (Day 22)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model3)
Experiment 5 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.60% (Day 22)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model5)
Experiment 6 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 22)	High HER2 expression (HER2+++; IHC 3+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model7)
Experiment 7 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 22)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model1)
Experiment 8 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 22)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model2)
Experiment 9 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 22)	Moderate HER2 expression (HER2++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 22 days.
In Vivo Model	Gastric cancer PDX model (PDX: Model4)

Experiment 1 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90.00 ng/mL	Low HER2 expression (HER2+; IHC 1+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with PBS, ADC (5 mg/kg), PD-1 antibody (10 mg/kg), or their combination (ADC+PD-1 antibody or ADC+PD-L1 antibody) for 10 days.
In Vivo Model	Triple-negative breast cancer cell line E0771-hHER2 xenograft model
In Vitro Model	Mammary gland malignant neoplasms	EO771 cells		CVCL_GR23
Experiment 2 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 ug/mL	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.30 ug/mL	High HER2 expression (HER2+++; IHC 3+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric tubular adenocarcinoma	SNU-216 cells		CVCL_3946
Experiment 4 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.80 ug/mL	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 5 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52.40 ug/mL	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The inhibitory activity of RC48 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with RC48 for 72 h.
In Vitro Model	Gastric carcinoma	HGC-27 cells		CVCL_1279

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.91 ng/mL	High HER2 expression (HER2+++)
Method Description	To test the anti-tumor effect of single drug, SK-BR-3, NCI-N87 and SK-OV-3 cells were selected for viability analysis following 72 h incubation with or without RC48ADC which was dispersed in a concentration gradient.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.28 ng/mL	High HER2 expression (HER2+++)
Method Description	To test the anti-tumor effect of single drug, SK-BR-3, NCI-N87 and SK-OV-3 cells were selected for viability analysis following 72 h incubation with or without RC48ADC which was dispersed in a concentration gradient.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.54 ng/mL	High HER2 expression (HER2+++)
Method Description	To test the anti-tumor effect of single drug, SK-BR-3, NCI-N87 and SK-OV-3 cells were selected for viability analysis following 72 h incubation with or without RC48ADC which was dispersed in a concentration gradient.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Objective Response Rate (ORR)	73.30%
Patients Enrolled	Histologically documented locally advanced/metastatic urothelial carcinoma (la/mUC) (including squamous differentiation and mixed cell types), an Eastern Cooperative Oncology Group performance status score of 0 or 1 (on a 5-point scale; higher scores indicate greater disability), and an investigator-assessed life expectancy of 3 or more months.
Administration Dosage	1.25 mg/kg once daily on days 1 and 8 intravenously once daily in 3-week cycles.
Related Clinical Trial
NCT Number	NCT04223856	Phase Status	Phase 3
Clinical Description	An open-label, randomized, controlled phase 3 study of enfortumab vedotin in combination with pembrolizumab versus chemotherapy alone in previously untreated locally advanced or metastatic urothelial cancer.
Primary Endpoint	Safety: Seven patients (15.60%) experienced a serious TRAE, with no serious TRAE occurring more than once. TRAEs led to dose reductions in 14 (31.10%) patients and discontinuations in 11 (24.40%) patients and were not mutually exclusive. Peripheral sensory neuropathy was the most common TRAE leading to either dose reduction (six patients, 13.30%) or treatment discontinuation (four patients, 8.90%). No patients discontinued therapy because of a skin reaction or hyperglycemia. One patient (2.20%) died because of a TRAE (multiple organ dysfunction syndrome).    Click to Show/Hide
Other Endpoint	The confirmed objective response rate after a median of nine cycles was 73.30% with a complete response rate of 15.60%. The median DOR and median OS were 25.60 months and 26.10 months, respectively.
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Objective Response Rate (ORR)	44.00%	High Nectin-4 expression (NECTIN4+++)
Patients Enrolled	Locally advanced or metastatic urothelial carcinoma who were previously treated with platinum chemotherapy and antiPD-1/L1 therapy.
Administration Dosage	1.25 mg/kg (intravenously on days 1, 8, and 15 of every 28-day cycle).
Related Clinical Trial
NCT Number	NCT03219333	Phase Status	Phase 2
Clinical Description	A single-arm, open-label, multicenter study of enfortumab vedotin (ASG-22CE) for Treatment of patients with locally advanced or metastatic urothelial cancer who previously received immune checkpoint inhibitor (CPI) Therapy.
Primary Endpoint	Confirmed objective response rate was 44.00% (95% CI, 35.10% to 53.20%), including 12.00% complete responses.
Other Endpoint	Median duration of response was 7.60 months (range, 0.95 to 11.30 months).
Experiment 3 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Objective Response Rate (ORR)	51.68%	High Nectin-4 expression (NECTIN4+++)
Patients Enrolled	Locally advanced or metastatic urothelial carcinoma previously treated with PD-1 or PD-L1 inhibitors; an Eastern Cooperative Oncology Group performance status score of 2 or less who were considered ineligible for cisplatin at enrolment and who had not received platinum-containing chemotherapy in the locally advanced or metastatic setting.
Administration Dosage	Intravenously at a dose of 1.25 mg/kg on days 1, 8, and 15 of every 28-day cycle.
Related Clinical Trial
NCT Number	NCT03219333	Phase Status	Phase 2
Clinical Description	A single-arm, open-label, multicenter study of enfortumab vedotin (ASG-22CE) for treatment of patients with locally advanced or metastatic urothelial cancer who previously received immune checkpoint inhibitor (CPI) therapy.
Primary Endpoint	The confirmed objective response rate was 51.68% (46 of 89 patients; 95% CI 41.00-62.00), with 18 (20.22%) of 89 patients achieving a complete response and 28 (31.46%) achieving a partial response.
Other Endpoint	Duration of response, progression-free survival, objective response rate, overall survival, safety, and tolerability, plasma or serum pharmacokinetic parameters of enfortumab vedotin, MMAE, and total antibody, and incidence of antitherapeutic antibody to enfortumab vedotin.
Experiment 4 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Objective Response Rate (ORR)	35.30%	Moderate Nectin-4 expression (NECTIN4++)
Patients Enrolled	Histologically confirmed, locally advanced or metastatic transitional cell carcinoma of the urothelium (ie, cancer of the bladder, renal pelvis, ureter, or urethra), or UC with squamous differentiation or mixed cell types and an Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.
Administration Dosage	1.00 mg/kg (Arm A) or 1.25 mg/kg (Arm B) on Days 1, 8, and 15 of each 28-day cycle.
Related Clinical Trial
NCT Number	NCT03070990	Phase Status	Phase 1
Clinical Description	An open-label, randomized, phase 1 safety and pharmacokinetic study of enfortumab vedotin (ASG-22CE) in Japanese patients with locally advanced or metastatic urothelial carcinoma.
Primary Endpoint	Safety/tolerability of EV, EV PK profile.
Experiment 5 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Objective Response Rate (ORR)	43.00%	High Nectin-4 expression (NECTIN4+++)
Patients Enrolled	Nectin-4positive solid tumors, including mUC, who progressed on 1 prior chemotherapy regimen or who were ineligible for cisplatin chemotherapy.
Administration Dosage	Weight-based doses (0.50, 0.75, 1.00, and 1.25 mg/kg) through 30-minute infusion on days 1, 8, and 15 of a 28-day cycle.
Related Clinical Trial
NCT Number	NCT02091999	Phase Status	Phase 1
Clinical Description	A phase 1 study of the safety and pharmacokinetics of escalating doses of ASG-22CE given as monotherapy in subjects with metastatic urothelial cancer and other malignant solid tumors that express nectin-4.
Primary Endpoint	The determination of safety/tolerability, recommended phase II dose (RP2D), and pharmacokinetic (PK) profile of EV.
Other Endpoint	Antitumor activity,including confirmed investigator-assessed ORR (RECIST version 1.1), duration of response (DoR), progression-free survival (PFS), and overall survival (OS).
Experiment 6 Reporting the Activity Date of This ADC					[72]
Patients Enrolled	Histologically or cytologically confirmed urothelial carcinoma (including differentiation in squamous cells or in multiple cell types), radiologically documented metastatic or unresectable locally advanced disease at baseline, and an Eastern Cooperative Oncology Group (ECOG) performance-status score of 0 or 1 (scores range from 0 to 4, with higher scores indicating greater disability).    Click to Show/Hide
Administration Dosage	Intravenous infusion over 30 minutes on days 1, 8, and 15 of a 28-day cycle.
Related Clinical Trial
NCT Number	NCT03474107	Phase Status	Phase 3
Clinical Description	An open-label, randomized phase 3 study to evaluate enfortumab vedotin vs chemotherapy in subjects with previously treated locally advanced or metastatic urothelial cancer (EV-301).
Primary Endpoint	Overall survival was prolonged with enfortumab vedotin compared with chemotherapy (HR=0.70 [95% CI: 0.56-0.89];.
Other Endpoint	Median overall survival: 12.88 vs 8.97 months, respectively). Progression-free survival was also longer in the enfortumab vedotin group compared with the chemotherapy group (HR=0.62 [95% CI: 0.51-0.75]; P<0.00001; median progression-free survival: 5.55 vs 3.71 months, respectively).

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.80% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a bladder cancer cell with Nectin-4 high expression, dosed every 4 days at 0.4 mg/kg for 5 times.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B1)
Experiment 2 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.90% (Day 24)	Moderate Nectin-4 expression (NECTIN4++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a pancreatic cancer cell with Nectin-4 moderate expression, dosed every 4 days at 1 mg/kg for 6 times.
In Vivo Model	Pancreatic cancer PDX model (PDX: AG-Panc4)
Experiment 3 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.00% (Day 24)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a breast cancer cell with Nectin-4 high expression, dosed every 4 days at 1 mg/kg for 6 times.
In Vivo Model	Breast cancer PDX model (PDX: AG-Br7)
Experiment 4 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.80% (Day 24)	Moderate Nectin-4 expression (NECTIN4++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a pancreatic cancer cell with Nectin-4 moderate expression, dosed every 4 days at 3 mg/kg for 6 times.
In Vivo Model	Pancreatic cancer PDX model (PDX: AG-Panc4)
Experiment 5 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.70% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a bladder cancer cell with Nectin-4 high expression, dosed every 4 days at 0.8 mg/kg for 5 times.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B1)
Experiment 6 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80% (Day 24)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a breast cancer cell with Nectin-4 high expression, dosed every 4 days at 3 mg/kg for 6 times.
In Vivo Model	Breast cancer PDX model (PDX: AG-Br7)
Experiment 7 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in orthotopic PDX models of a breast cancer cell with Nectin-4 high expression, established in mammary fat pads of SCID mice, dosed single 10 mg/kg.
In Vivo Model	Breast cancer orthotopic PDX model (PDX: AG-Br7)
Experiment 8 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.70% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in orthotopic PDX models of a breast cancer cell with Nectin-4 high expression, established in mammary fat pads of SCID mice, dosed twice 5 mg/kg.
In Vivo Model	Breast cancer orthotopic PDX model (PDX: AG-Br7)
Experiment 9 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a bladder cancer cell with Nectin-4 high expression, single 4 mg/kg dose.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B1)

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.00% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a lung adenocarcinoma cell with Nectin-4 high expression, dosed every 4 days at 1 mg/kg for 5 times.
In Vivo Model	NCI-H322M CDX model
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H322M cells		CVCL_1557
Experiment 2 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.60% (Day 18)	High Nectin-4 expression (NECTIN4+++)
Method Description	AGS-22M6E induces efficient tumor cell killing in PDX models of a lung adenocarcinoma cell with Nectin-4 high expression, dosed every 4 days at 3 mg/kg for 5 times.
In Vivo Model	NCI-H322M CDX model
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H322M cells		CVCL_1557

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.20 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 2 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.40 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 3 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.70 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 4 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37.80 ng/mL
Method Description	The inhibitory activity of AGS-22M6, AGS-22M6E ADC, and an isotype control ADC were added to various cancer cell lines in vitro and cell viability was measured after 5 days.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Objective Response Rate (ORR)	54.00%
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma or relapsed or refractory grade 13a follicular lymphoma.
Administration Dosage	Either rituximab (375 mg/m2) followed by pina (2.4 mg/kg) every 21 days, or rituximab (375 mg/m2) followed by pola (2.4 mg/kg) every 21 days until disease progression or unacceptable toxicity up to 1 year.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of pinatuzumab vedotin (DCDT2980S) in combination with rituximab or polatuzumab vedotin (DCDS4501A) in combination with rituximab and a non-randomized phase 1b/2 evaluation of polatuzumab vedotin in combination with obinutuzumab in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma.    Click to Show/Hide
Primary Endpoint	Among patients with refractory diffuse large B-cell lymphoma, complete responses and median overall survival compares favourably with immunochemotherapy regimens reported in the SCHOLAR-1 study, in which 7.00% of patients achieved a complete response and a median overall survival of 6.30 months was observed.
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Objective Response Rate (ORR)	41.50% (pola + BR)
Patients Enrolled	Patients aged 18 years were eligible if they had histologically confirmed R/R DLBCL (excluding transformed follicular lymphoma), received 1 prior line of therapy, had an Eastern Cooperative Oncology Group performance status of 0 to 2, and were considered transplant ineligible by the treating physician or experienced treatment failure with prior autologous SCT.    Click to Show/Hide
Administration Dosage	Bendamustine 90 mg/m2 intravenously (IV) on days 2 and 3 of cycle 1, and days 1 and 2 of subsequent cycles, plus rituximab IV (375 mg/m2 on day 1 of each cycle); polatuzumab vedotin received 1.80 mg/kg IV on day 2 of cycle 1, and day 1 of subsequent cycles; up to six 21-day cycles.
Related Clinical Trial
NCT Number	NCT02257567	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 study evaluating the safety, tolerability and anti-tumor activity of polatuzumab vedotin in combination with rituximab (R) or obinutuzumab (G) plus bendamustine (B) in relapsed or refractory follicular or diffuse large B-cell lymphoma.
Primary Endpoint	With an additional 27 months of follow-up in the randomized pola + BR arm was 62.50% vs 25.00%; best CR rate was 52.50% vs 22.50%.
Other Endpoint	The median IRC-assessed PFS (95% CI) was 9.20 months (6.00-13.90) with pola + BR vs 3.70 months (2.10-4.50) with BR (HR, 0.39; 95% CI, 0.23-0.66); median investigator-assessed PFS was 7.50 vs 2.00 months (HR, 0.33; 95% CI, 0.20-0.56) with pola + BR and BR, respectively. Median OS (95% CI) was 12.40 months (9.00-32.00) vs 4.70 months (3.70-8.30) with pola + BR vs BR (HR, 0.42; 95% CI, 0.24-0.72). The 24-month OS probability was 38% (95% CI, 22.50-53.90) with pola + BR vs 17.0% (3.60-30.40) with BR. The 24-month PFS probability was 28.40% (95% CI, 13.9-43.0) with pola + BR vs 9.10% (95% CI, 0.00-18.90) with BR.The median DOR was 9.50 months (95% CI, 7.90-12.10) by IRC assessment and 8.70 months (95% CI, 5.90-12.10) by investigator assessment. The median IRC-assessed PFS was 6.6 months (95% CI, 5.10-9.20). Median OS was 12.50 months (95% CI, 8.20-23.10); the 12-month OS probability was 50.20% (95% CI, 40.40-60.10).    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Objective Response Rate (ORR)	76.09%
Patients Enrolled	CD20-positive relapsed or refractory follicular lymphoma (excluding grade 3b) and Eastern Cooperative Oncology Group performance status of 2 or less who had previously received anti-CD20-containing chemotherapy were eligible for inclusion.
Administration Dosage	Six 28-day cycles of induction treatment with intravenous obinutuzumab 1000 mg (all cohorts), and intravenous polatuzumab vedotin and oral lenalidomide (Celgene, Summit, NJ, USA) in the following doses: 14 mg/kg polatuzumab vedotin and 10 mg lenalidomide (cohort 1); 18 mg/kg polatuzumab vedotin and 10 mg lenalidomide (cohort 2); 14 mg/kg polatuzumab vedotin and 15 mg lenalidomide (cohort 3); 18 mg/kg polatuzumab vedotin and 15 mg lenalidomide (cohort 4); 14 mg/kg polatuzumab vedotin and 20 mg lenalidomide (cohort 5); and 18 mg/kg polatuzumab vedotin and 20 mg lenalidomide (cohort 6). Polatuzumab vedotin was administered on day 1, lenalidomide on days 1-21, and obinutuzumab on days 1, 8, and 15 of cycle one and day 1 of cycles two to six of each 28-day cycle.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02600897	Phase Status	Phase 1b/2
Clinical Description	A phase 1b/2 study evaluating the safety and efficacy of obinutuzumab in combination with polatuzumab vedotin and lenalidomide in patients with relapsed or refractory follicular lymphoma and rituximab in combination with polatuzumab vedotin and lenalidomide in patients with relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	According to the Independent Review Committeeassessment, 29 (63.04%) of 46 patients (90% CI 50.00-75.00) had acomplete response and 35 (76.09%) patients (90% CI 64.00-86.00) had an objective response, per Modified Lugano 2014 criteria. Independent Review Committee assessment showed that 33 (71.74%) patients (90% CI59.00-82.00) had a complete metabolic response at the end ofinduction per Modified Lugano 2014 criteria.    Click to Show/Hide
Other Endpoint	At data cut-off (median follow-up 26.70 months [IQR 22.20-31.30]),median progression-free survival had not been reached. As determined by the investigator, theprogression-free survival was 86.00% (95% CI 75.00-96.00) at 12 months and 67.00% (95% CI 51.00-83.00) at 24 months, and 11 (23.91%) of 46 patients had an event reported at the time of this analysis.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Objective Response Rate (ORR)	33.00% (FL patients treated with G-atezo-pola at pola doses of 1.4 mg/kg) 57.00% (FL patients treated with G-atezo-pola at pola doses of 1.8 mg/kg) 25.00% (DLBCL patients who received R-atezo-pola)
Patients Enrolled	R/R follicular lymphoma (FL); R/R diffuse large B-cell lymphoma (DLBCL).
Administration Dosage	FL patients received up to six 21-day cycles of obinutuzumab (1000 mg intravenously [IV], Day [D]1, D8, D15 of Cycle [C]1, and D1 of C26) and atezolizumab (1200 mg IV, D1 of C26) plus pola (1.40 or 1.80 mg/kg IV, D1 of C16). Subsequently, patients entered an expansion phase and received obinutuzumab and atezolizumab (same doses) plus pola at the RP2D (1.8 mg/kg). Patients who achieved at least stable disease at the end of induction (EOI; 68 weeks after D1C6) proceeded to obinutuzumab maintenance (1000 mg every 2 months) and atezolizumab (840 mg, D1 and D2 every month) for up to 2 years, or until progressive disease (PD). Unlike the FL cohort, the first seven DLBCL patients entered a safety run-in; once safety criteria were met, the cohort was expanded. All DLBCL patients received up to six 21-day cycles of rituximab (375 mg/m2 IV, D1 of C16), atezolizumab (1200 mg, D1 of C26), and pola (1.80 mg/kg, D1 of C16). Patients with at least a partial response (PR) at EOI (68 weeks after D1 of C6) received rituximab consolidation (375 mg/m2, D1 every 2 months) and atezolizumab (840 mg, D1 and D2 every month) for up to 8 months, or until PD.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02729896	Phase Status	Phase 1b
Clinical Description	A phase 1b/2 study evaluating the safety and efficacy of obinutuzumab in combination with atezolizumab plus polatuzumab vedotin in patients with relapsed or refractory follicular lymphoma and rituximab in combination with atezolizumab plus polatuzumab vedotin in patients with relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	At EOI, CR rates in FL patients treated with G-atezo-pola at pola doses of 1.40 mg/kg (N=3) and 1.80 mg/kg (N=7) were 33.00% and 14.00% , respectively. In DLBCL patients who received R-atezo-pola, the CR rate at EOI was 13.00%.
Other Endpoint	At EOI, ORR rates in FL patients treated with G-atezo-pola at pola doses of 1.40 mg/kg (N=3) and 1.80 mg/kg (N=7) were 33.00% and 57.00% , respectively. In DLBCL patients who received R-atezo-pola, the ORR rate at EOI was 25.00%.
Experiment 5 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Objective Response Rate (ORR)	42.86%
Patients Enrolled	Elapsed/refractory (R/R) diffuse large B-cell lymphoma (DLBCL) who received 1 prior line of therapy and were ineligible for autologous stem cell transplantation (ASCT) or experienced treatment failure with prior ASCT.
Administration Dosage	Pola 1.80 mg/kg intravenously (IV) on day 2 of cycle 1 and day 1 of subsequent cycles; bendamustine 90 mg/m2IV on days 2 and 3 of cycle 1 and then days 1 and 2 of subsequent cycles; rituximab 375 mg/m2IV on day 1 of each cycle. Three weeks of treatment was regarded as one cycle, and patients received up to six cycles of treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02257567	Phase Status	Phase 1
Clinical Description	A phase 1b/2 study evaluating the safety, tolerability and anti-tumor activity of polatuzumab vedotin in combination with rituximab (R) or obinutuzumab (G) plus bendamustine (B) in relapsed or refractory follicular or diffuse large B-cell lymphoma.
Primary Endpoint	2 patients (34.30%, 95% CI 19.1-52.2) achieved CR.
Other Endpoint	Seven of 12 patients who achieved CR completed six cycles of treatment. Fifteen patients (42.86%, 95% CI 26.30-60.70) achieved an overall response (12 patients CR; 3 patients PR). At a median followup of 5.40 months, median DOR, PFS, and EFS were 6.60 months, 5.20 months, and 5.10 months, respectively. Twentythree patients (65.71%) were alive, and median OS was not reached (95% CI 8.40-not evaluable [NE]).    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Complete Remission (CR)	57.60% (FL) 23.50% (DLBCL)
Patients Enrolled	R/R follicular lymphoma (FL) and R/R diffuse large B-cell lymphoma (DLBCL); the majority had an Eastern Cooperative Oncology Group performance score of 0 or 1.
Administration Dosage	Dose escalation FL cohorts (3 + 3 design); Dose escalation DLBCL cohorts (3 + 3 design); polatuzumab vedotin 1.80 mg/kg and venetoclax 800 mg.
Related Clinical Trial
NCT Number	NCT02611323	Phase Status	Phase 1
Clinical Description	A phase 1b/2 study evaluating the safety and efficacy of obinutuzumab in combination with polatuzumab vedotin and venetoclax in patients with relapsed or refractory follicular lymphoma and rituximab in combination with polatuzumab vedotin and venetoclax in patients with relapsed or refractory diffuse large B-cell lymphoma.
Primary Endpoint	The overall response rate (ORR) for patients with FL was 75.80%, with 57.60% of patients achieving a complete response (CR). All patients in FL cohort 6 treated at the identified RP2D dose combination achieved CR at EOI. The ORR observed for patients with DLBCL was 29.40%; 23.50% achieved CR. Similar trends were seen in the DLBCL cohorts, with higher response rates in patients treated at the RP2D (37.5% vs. 22.2%).    Click to Show/Hide
Experiment 7 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Complete Remission (CR)	50.00% (In the phase Ib pola-BR arm, EOT IRC-assessed) 40.00% (the randomly assigned cohort, IRC-assessed pola-BR) 17.50% (the randomly assigned cohort, IRC-assessed BR)
Patients Enrolled	Patients aged 18 years were eligible if they had biopsy-confirmed R/R DLBCL (excluding transformed lymphoma) after 1 prior line of therapy, an Eastern Cooperative Oncology Group (ECOG) performance status of 0-2, grade 1 peripheral neuropathy (PN), and were considered transplantation ineligible by the treating physician or experienced treatment failure with prior ASCT. Double- and triple-hit lymphomas were not excluded.    Click to Show/Hide
Administration Dosage	1.80 mg/kg IV on day 2 of cycle 1 and day 1 of subsequent cycles. Patients were treated for up to six 21-day cycles.
Related Clinical Trial
NCT Number	NCT01287741	Phase Status	Phase Ib/II
Clinical Description	A phase Ib/II, multicenter, open-label randomized trial comparing the efficacy of GA101 (RO5072759) in combination with CHOP (G-CHOP) versus rituximab and CHOP (R-CHOP) in previously untreated patients with CD20-positive diffuse large B-cell lymphoma (DLBCL).
Primary Endpoint	In the phase Ib pola-BR arm, EOT IRC-assessed CR rate was 50.00% (3/6), with all 3 patients remaining in remission at a median follow-up of 37.60 months (DOR, > 28.90 to 38.20 months).
Other Endpoint	After a median follow-up of 22.3 months, PFS, OS, and DOR were significantly improved with pola-BR versus BR. Consistent benefit in risk reduction was seen for IRC- and INV-assessed PFS (IRC: HR, 0.36; 95% CI, 0.21-0.63; INV: HR, 0.34; 95% CI 0.20-0.57) and for DOR (IRC: HR, 0.47; 95% CI, 0.19-1.14; INV: HR,0.44, 95% CI 0.20-0.95).
Experiment 8 Reporting the Activity Date of This ADC					[71]
Patients Enrolled	CD20-positive diffuse large B-cell lymphoma (DLBCL), had not received previous treatment for lymphoma, had an Eastern Cooperative Oncology Group performance status score of 0 to 2 (on a 5-point scale, with higher numbers indicating greater disability), had a baseline International Prognostic Index (IPI) score between 2 and 5 (on a 5-level prognostic scale, with higher numbers indicating a poorer prognosis), and had adequate hematologic, renal, hepatic, and cardiac function, regardless of the cell of origin or the presence of rearrangements in MYC, BCL2, BCL6, or a combination of these.    Click to Show/Hide
Administration Dosage	Eight 21-day cycles of treatment were planned. During the first six cycles, patients received either pola-R-CHP or R-CHOP. On day 1 of each cycle, patients received either intravenous polatuzumab vedotin at a dose of 1.80 mg per kilogram of body weight and a placebo matching intravenous vincristine (pola-R-CHP group) or a placebo matching polatuzumab vedotin and intravenous vincristine at a dose of 1.40 mg per square meter of body-surface area (maximum of 2 mg) (R-CHOP group), plus intravenous doses of rituximab (375 mg per square meter), cyclophosphamide (750 mg per square meter), and doxorubicin (50 mg per square meter). All the patients also received oral prednisone at a dose of 100 mg once daily on days 1 through 5 of each of the first six cycles. During cycles 7 and 8, patients in both groups received rituximab monotherapy at a dose of 375 mg per square meter.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03274492	Phase Status	Phase 3
Clinical Description	A phase 3, multicenter, randomized, double-blind, placebo-controlled trial comparing the efficacy and safety of polatuzumab vedotin in combination with rituximab and CHP (R-CHP) versus rituximab and CHOP (R-CHOP) in previously untreated patients with diffuse large B-cell lymphoma.
Primary Endpoint	For the pola-R-CHP group, 2 years FPS=76.70% (95% CI, 72.70-80.80). For the R-CHOP group, 2 years FPS=70.20% (95% CI, 65.80-74.60).
Other Endpoint	The relative risk of events was lower in the pola-R-CHP group than in the R-CHOP group (2-year event-free survival, 75.60% [95% CI, 71.50 to 79.70] and 69.40% [95% CI, 65.00 to 73.80%], respectively.
Experiment 9 Reporting the Activity Date of This ADC					[78]
Patients Enrolled	Non Hodgkin lymphoma (NHL) or chronic lymphocytic leukemia (CLL) expected to express CD79B (confirmation of CD79B expression was not required) and for whom no suitable therapy of curative intent or higher priority existed from 13 centres.
Administration Dosage	0.124 mg/kg every 21 days.
Related Clinical Trial
NCT Number	NCT01290549	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, phase 1 trial of the safety and pharmacokinetics of escalating doses of DCDS4501A in patients with relapsed or refractory B-cell non-Hodgkins lymphoma and chronic lymphocytic leukemia and DCDS4501A in combination with rituximab in patients with relapsed or refractory B-cell non-Hodgkins lymphoma.
Primary Endpoint	Polatuzumab vedotin has an acceptable safety and tolerability profile in patients with NHL but not in those with CLL. Among 45 patients with NHL treated at the recommended phase 2 dose of single-agent polatuzumab vedotin, median progressionfree survival was 5.70 months (95% CI 3.00-7.90) and median duration of response was 6.2 months (95% CI 3.3-14.1). In patients with diffuse large B-cell lymphoma treated at the recommended phase 2 dose of single-agent polatuzumab, median progression-free survival was 5.00 months (95% CI 2.30-6.80) and median duration of response was 5.20 months (95% CI 2.40-13.10).    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.60% (Day 28)	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 1 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 2 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.40% (Day 28)	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 2 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 3 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 6.60% (Day 14)	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 0.1 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 4 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.10% (Day 28)	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 4 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 5 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.20% (Day 14)	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 6 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.90% (Day 28)	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 8 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 7 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.30% (Day 14)	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 1 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 8 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.90% (Day 28)	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 12 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 9 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10% (Day 14)	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 1.5 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 10 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.90% (Day 28)	High CD22 expression (CD22+++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 16 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 11 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 14)	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 2 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711
Experiment 12 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 14)	Moderate CD22 expression (CD22++)
Method Description	Cells were inoculated subcutaneously into the flanks of female CB17 ICR severe combined immunodeficient (SCID) mice. When mean tumor size reached desired volume,the mice were divided into groups of 7 to 9 mice with the same mean tumor size and dosed intravenously via the tail vein with ADCs or antibodies. Rituximab was dosed at 30 mg/kg intraperitoneally (i.p.). Polatuzumab vedotin was administered as a single injection at 4 mg/kg.    Click to Show/Hide
In Vivo Model	B-cell lymphoma CDX model
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Objective Response Rate (ORR)	30.00%
Patients Enrolled	Patients with diffuse large B-cell lymphoma (DLBCL), PET-positive disease, and ECOG PS of 0-2. Pts must have received 2 prior lines of therapy.
Administration Dosage	2.50 mg/kg IV Q3W.
Related Clinical Trial
NCT Number	NCT05144841	Phase Status	Phase 2
Clinical Description	A phase 2 open-label clinical study to evaluate the efficacy and safety of zilovertamab vedotin (MK-2140) in participants with relapsed or refractory diffuse large B-cell lymphoma (waveline-004).
Experiment 2 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Objective Response Rate (ORR)	47.00% (MCL) 60.00% (DLBCL)
Patients Enrolled	Patients with tumor histologies of mantle cell lymphoma (MCL), chronic lymphocytic leukemia, diffuse large B-cell lymphoma (DLBCL). Patients had received a median of four previous drug and/or cellular therapies.
Administration Dosage	2.50 mg/kg every 3 week.
Related Clinical Trial
NCT Number	NCT03833180	Phase Status	Phase 1
Clinical Description	A phase 1 dose-escalation and cohort-expansion study of VLS-101 in subjects with hematological malignancies (waveline-001).
Experiment 3 Reporting the Activity Date of This ADC					[107]
Patients Enrolled	Patients with diffuse large B-cell lymphoma (DLBCL) after 1 line of prior therapy (cohort A) or 2 lines of prior therapy (cohort B).
Administration Dosage	ZV (1.50, 1.75, 2.00, 2.25, and 2.50 mg/kg) with gemcitabine-oxaliplatin + rituximab (R-GemOx).
Related Clinical Trial
NCT Number	NCT05139017	Phase Status	Phase 2/3
Clinical Description	A phase 2/3 multicenter, open-label, randomized, active-control study of zilovertamab vedotin (MK-2140) in combination with standard of care in participants with relapsed or refractory diffuse large B-cell lymphoma (waveline-003).
Experiment 4 Reporting the Activity Date of This ADC					[109]
Patients Enrolled	Patients with mantle cell lymphoma (MCL), Richter's transformation (RT), chronic lymphocytic leukemia (CLL), or follicular lymphoma (FL), relapsed or refractory (R/R) disease, ECOG performance status of 0 to 2.
Administration Dosage	ZV 2.0 to 2.50 mg/kg IV Q3W.
Related Clinical Trial
NCT Number	NCT05458297	Phase Status	Phase 2
Clinical Description	A multicenter, open-label, phase 2 basket study to evaluate the safety and efficacy of MK-2140 as a monotherapy and in combination in participants with aggressive and indolent B-cell malignancies.
Experiment 5 Reporting the Activity Date of This ADC					[110]
Patients Enrolled	Patients with previously untreated histologically confirmed diffuse large B-cell lymphoma (DLBCL), PET-positive and ECOG PS of 0 or 1.
Administration Dosage	ZV was 1.75 mg/kg (modified to 1.50, 2.00, 2.25, or 2.50 mg/kg) administered as an intravenous infusion every 3 weeks (Q3W) in combination with R-CHP.
Related Clinical Trial
NCT Number	NCT05406401	Phase Status	Phase 2
Clinical Description	A multicenter, open-label, phase 2 dose escalation and confirmation, and efficacy expansion study of zilovertamab vedotin (MK-2140) in combination with r-chp in participants with DLBCL (waveline).
Experiment 6 Reporting the Activity Date of This ADC					[119]
Patients Enrolled	Patients with locally advanced or metastatic urothelial carcinoma (mUC) whose disease is resistant to treatment with programmed cell death-1/ligand 1 (PD-1/L1) inhibitors.
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NCT Number	NCT05562830	Phase Status	Phase 1/2
Clinical Description	A phase 1/2 open-label rolling-arm umbrella platform study of investigational agents with or without pembrolizumab in participants with PD-1/L1 refractory locally advanced or metastatic urothelial carcinoma (keymaker-u04): substudy 04a.
Experiment 7 Reporting the Activity Date of This ADC					[123]
Related Clinical Trial
NCT Number	NCT04504916	Phase Status	Phase 1
Clinical Description	A phase 2 study of VLS-101 in patients with solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 30)	Negative ROR1 expression (ROR1-)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 2 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 30)	Negative ROR1 expression (ROR1-)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 3 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80% (Day 47)	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: IP867/17)
Experiment 4 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.90% (Day 57)	Moderate ROR1 expression (ROR1++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 5 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 47)	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: IP867/17)
Experiment 6 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 47)	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 2.5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 7 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 47)	High ROR1 expression (ROR1+++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)
Experiment 8 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 57)	Moderate ROR1 expression (ROR1++)
Method Description	VLS-101 induces efficient tumor cell killing in cell line-derived models of IP867/17 and RS1316 cells with UC-961 expression with high expression. After palpable tumors were evident (tumor volume of 0.2 cm3),animals were randomly assigned to vehicle,VLS 101 5 mg/kg.
In Vivo Model	Richter syndrome PDX model (PDX: RS9737)

Experiment 1 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Objective Response Rate (ORR)	34.70%
Patients Enrolled	Advanced/metastatic HER2-low expressing breast cancer that failed standard therapies.
Administration Dosage	MRG002 was administered intravenously once every 3 weeks at the dose of 2.60 mg/kg, until disease progression or unacceptable toxicity which ever occurred first.
Related Clinical Trial
NCT Number	NCT04742153	Phase Status	Phase 2
Clinical Description	A multicenter, non-randomized, open-label phase 2 clinical study to evaluate the efficacy and safety of MRG002 in the treatment of patients with HER2-low locally advanced or metastatic breast cancer (BC).
Experiment 2 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Objective Response Rate (ORR)	65.00%
Patients Enrolled	Histologically HER2-positive (IHC 2+ or 3+) UC pts confirmed by a central-laboratory, ECOG PS 0-1, prior received 1 standard treatment.
Administration Dosage	Receive MRG002 at a dose of 2.60 mg/kg or 2.20 mg/kg administered by intravenous infusion every 3 weeks.
Related Clinical Trial
NCT Number	NCT04839510	Phase Status	Phase 2
Clinical Description	An open-label, single-arm, multi-center, phase 2 clinical study of MRG002 in the treatment of patients with HER2-positive unresectable locally advanced or metastatic urothelium cancer.
Experiment 3 Reporting the Activity Date of This ADC					[106]
Related Clinical Trial
NCT Number	NCT05754853	Phase Status	Phase 3
Clinical Description	An open-label, randomized, multi-center, phase 3 clinical study of MRG002 versus investigator's choice of chemotherapy in the treatment of patients with HER2-positive unresectable locally advanced or metastatic urothelial cancer previously treated with platinum-based chemotherapy and PD-1/PD-L1 inhibitors.
Experiment 4 Reporting the Activity Date of This ADC					[108]
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NCT Number	NCT04924699	Phase Status	Phase 2/3
Clinical Description	A study of MRG002 in the treatment of patients with HER2-positive unresectable locally advanced or metastatic breast cancer.
Experiment 5 Reporting the Activity Date of This ADC					[111]
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NCT Number	NCT05263869	Phase Status	Phase 2
Clinical Description	An open-label, multi-center, single-arm phase 2 clinical study to evaluate the efficacy and safety of MRG002 in advanced HER-2 positive breast cancer patients previously treated with trastuzumab and TKIs (Magic-009).
Experiment 6 Reporting the Activity Date of This ADC					[112]
Related Clinical Trial
NCT Number	NCT05141786	Phase Status	Phase 2
Clinical Description	An open-label, multi-center, non-randomized phase 2 clinical study to evaluate the efficacy and safety of MRG002 in patients With HER2-mutated unresectable/metastatic non-small cell lung cancer (NSCLC).
Experiment 7 Reporting the Activity Date of This ADC					[113]
Related Clinical Trial
NCT Number	NCT05141747	Phase Status	Phase 2
Clinical Description	An open-label, multi-center, phase 2 clinical study to evaluate the safety, efficacy and pharmacokinetics of MRG002 in patients with HER2-positive/HER2-low locally advanced or metastatic gastric/ gastroesophageal junction cancer.
Experiment 8 Reporting the Activity Date of This ADC					[114]
Related Clinical Trial
NCT Number	NCT04837508	Phase Status	Phase 2
Clinical Description	An open-label, single-arm, multi-center, phase 2 clinical study of MRG002 in the treatment of patients with HER2-positive unresectable, locally advanced or metastatic biliary tract cancer.
Experiment 9 Reporting the Activity Date of This ADC					[120]
Related Clinical Trial
NCT Number	NCT05338957	Phase Status	Phase 1/2
Clinical Description	An open-label, multi-center, phase 1/2 dose escalation and expansion study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of MRG002 in combination with HX008 in patients with HER2-expressed advanced malignant solid tumors.
Experiment 10 Reporting the Activity Date of This ADC					[121]
Related Clinical Trial
NCT Number	NCT04492488	Phase Status	Phase 1/2
Clinical Description	An open-label, multi-center phase 1/2 dose escalation and expansion study to assess the safety, efficacy and pharmacokinetics of MRG002 in patients with HER2-positive advanced solid tumors and locally advanced or metastatic gastric/gastroesophageal junction (GEJ) cancer.
Experiment 11 Reporting the Activity Date of This ADC					[124]
Related Clinical Trial
NCT Number	NCT04941339	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, multi-center, first in human, dose escalation and expansion study to assess the safety, tolerability, efficacy and pharmacokinetics of MRG002 in patients with HER2 positive advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0.00% (Day 21)	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#151)
Experiment 2 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	10.00% (Day 21)	Low HER2 expression (HER2+; IHC 1+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#395)
Experiment 3 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	17.00% (Day 21)	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#239)
Experiment 4 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	19.00% (Day 21)	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#053)
Experiment 5 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	41.00% (Day 21)	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#240)
Experiment 6 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.10% (Day 63)	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#046)
Experiment 7 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.00% (Day 56)	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#179)
Experiment 8 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.40% (Day 35)	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 9 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.90% (Day 24)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 10 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	84.00% (Day 21)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)
Experiment 11 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.90% (Day 70)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#197)
Experiment 12 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90.00% (Day 21)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#069)
Experiment 13 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 63)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#046)
Experiment 14 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10% (Day 56)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#179)
Experiment 15 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 70)	High HER2 expression (HER2+++; IHC 3+)
In Vivo Model	HER2-positive breast cancer PDX model (PDX: BC#197)
Experiment 16 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Low HER2 expression (HER2+; IHC 1+)
In Vivo Model	HER2-positive gastric cancer PDX model (PDX: STO#410)

Experiment 1 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.70% (Day 36)	Moderate HER2 expression (HER2++)
In Vivo Model	HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.20% (Day 36)	High HER2 expression (HER2+++)
Method Description	MRG-002 induces efficient tumor cell killing in PDX models of breast cancer or gastric cancer tissues with HER2 expression,administered with vehicle,MRG002,HX008 or MRG002 + HX008 combo intravenously.
In Vivo Model	HER2-positive breast cancer BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 36)	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive breast cancer BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 36)	Moderate HER2 expression (HER2++; IHC 2+)
In Vivo Model	HER2-positive breast cancer BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 36)	High HER2 expression (HER2+++)
In Vivo Model	HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 36)	High HER2 expression (HER2+++)
In Vivo Model	HER2-positive gastric cancer NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM
Method Description	The inhibitory activity of MRG-002 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated with MRG-002 for 96±2 hrs.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Objective Response Rate (ORR)	7.40%
Patients Enrolled	Advanced non-small cell lung cancer (NSCLC).
Administration Dosage	Teliso-V Q2W (1.60, 1.90, or 2.20 mg/kg, intravenous) with nivolumab (3 mg/kg, or 240 mg, or per locally approved label, intravenously).
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Most patients (97.30%, n=36) experienced one or more TEAE, with 23 (62.16%) reporting TEAEs grades 3 or higher. TEAEs considered possibly related to Teliso-V were reported in 78.38% (n=29) of patients; 32.43% (n=12) were grade greater than or equal to 3.
Other Endpoint	Combination therapy with Teliso-V plus nivolumab was well tolerated in patients with c-Met-+NSCLC with limited antitumor activity. The ORR was 7.40% (95% CI: 0.90-24.30), with two patients (PD-L1+, n =1; PD-L1-, n=1) having a confirmed PR.Overall, 66.67% of patients (16 of 24) had evidence of tumor size reduction; three (12.5%) reported a greater than 30% reduction in target lesion. The overall median PFS (95% CI) was 7.20 months (3.30-8.90); 7.20 months(1.50-not reached [NR]) for PD-L1 patients, 4.50 months(1.50-NR) for PD-L1- patients, and NR (2.00-NR) for PD-L1-unk patients. The objective response rate was 7.40%, with two patients having a confirmed partial response. Overall median progression-free survival was 7.20 months.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Objective Response Rate (ORR)	23.00% (all) 28.00% (in once every 2 weeks cohorts all) 18.00% (in once every 3 weeks cohorts) 18.00% (nonsquamous NSCLC) 31.00% (in once every 2 weeks cohorts nonsquamous NSCLC) 6.00% (in once every 3 weeks cohorts nonsquamous NSCLC) 43.00% (squamous NSCLC)
Patients Enrolled	Non-small cell lung cancer (NSCLC) and c-Met H-score 150 (c-Met+) or MET amplification/exon 14 skipping mutations.
Administration Dosage	Intravenously once every 3 weeks (0.15-3.30 mg/kg) or once every 2 weeks (1.60-2.20 mg/kg).
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Four objective responses (ORR = 26.70%; 95% CI, 7.80-55.10) were observed in this subgroup, 3 in once every 2 weeks (ORR = 43.00%; 95% CI, 9.90-81.60), and 1 in once every 3 weeks (ORR = 13.00%; 95% CI, 0.30-52.70).
Other Endpoint	The median PFS in once every 2 weeks cohorts was 8.00 months (range, 1.20-9.10) and the median treatment duration was 19.60 weeks (range, 0.10-60.10).
Experiment 3 Reporting the Activity Date of This ADC					[101]
Efficacy Data	Objective Response Rate (ORR)	30.55% (for all efficacy-evaluable patients) 32.10% (for EGFR-M+ patients) 52.60% (of EGFR-M+ patients, those who were c-Met high)
Patients Enrolled	Advanced non-small cell lung cancer (measurable per Response Evaluation Criteria in Solid Tumors v1.1) not amenable to resection or other approved therapies until disease progression, death, or withdrawal of consent.
Administration Dosage	Teliso-V (2.70 mg/kg once every 21 days) plus erlotinib (150 mg once daily) until disease progression, death, or withdrawal of consent.
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	OrR for all efficacy-evaluable patients was 30.55% (11/36; 95% CI, 16.30 to 48.10), and DCR was 86.11% (31/36; 95% CI, 70.5 to 95.3). Median PFS for all efficacy-evaluable patients was 5.90 months (95% CI, 2.80 to not reached [NR]).
Other Endpoint	For EGFR-M+ patients (n = 28), ORR was 32.14% (9/28; 95% CI, 15.90 to 52.40), with one CR (3.57%) and eight PR (28.57%). DCR was 85.71% (24/28; 95% CI, 67.30 to 96.00) and median PFS was 5.90 months (95% CI, 2.80 to NR). Median PFS was 3.70 months (95% CI, 1.40 to NR) for T790M+ patients, compared with 6.80 months (95% CI, 4.30 to NR) for non-T790M+ patients. Of EGFR-M+ patients, those who were c-Met high (n = 15) had an ORR of 52.60%. Median PFS was 6.80 months for non-T790M+ and for those whose T790M status was unknown, versus 3.70 months for T790M+.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[101]
Efficacy Data	Objective Response Rate (ORR)	30.60% (for all efficacy-evaluable patients) 32.18% (for EGFR-M+ patients) 52.60% (of EGFR-M+ patients, those who were c-Met high)
Patients Enrolled	Advanced non-small cell lung cancer (measurable per Response Evaluation Criteria in Solid Tumors v1.1) not amenable to resection or other approved therapies until disease progression, death, or withdrawal of consent.
Administration Dosage	Teliso-V (2.70 mg/kg once every 21 days) plus erlotinib (150 mg once daily) until disease progression, death, or withdrawal of consent.
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	Median PFS=5.90 months (95% CI, 2.80 to not reached). ORR for EGFR-M+ patients = 32.18% (n=28). EGFR-M+ patients ORR = 52.60%.
Other Endpoint	Median PFS=6.80 months for non-T790M+.
Experiment 5 Reporting the Activity Date of This ADC					[104]
Efficacy Data	Objective Response Rate (ORR)	71.70% (plus lenalidomide) 70.60% (plus pomalidomide)
Patients Enrolled	Relapsed or refractory multiple myeloma, and ECOG performance status or Zubrod score of 2 or below, received indatuximab ravtansine with lenalidomide and dexamethasone (indatuximab ravtansine plus lenalidomide) had failure of at least one previous therapy.
Administration Dosage	Intravenously on days 1, 8, and 15 of each 28-day cycle in dose of 100 mg/m2 plus lenalidomide or pomalidomide and dexamethasone.
Related Clinical Trial
NCT Number	NCT01638936	Phase Status	Phase 1
Clinical Description	A phase 1/2a multi-dose escalation study of BT062 in combination with lenalidomide or pomalidomide and dexamethasone in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 6 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Objective Response Rate (ORR)	75.00%
Patients Enrolled	MA advanced GEC.
Administration Dosage	15 mg/kg IV, once every 3 weeks.
Related Clinical Trial
NCT Number	NCT01472016	Phase Status	Phase 1
Clinical Description	A multi-center, phase 1/1b, open-label, dose escalation study of ABT-700, a monoclonal antibody in subjects with advanced solid tumors.
Primary Endpoint	Among these patients, three achieved a partial response and one had progressive disease as best response (ORR=75.00%). The duration of disease control in responders ranged from 18-27 weeks and the median duration of response was 16.10 weeks. The median progression- free survival in MET-amplified patients was 17.90 weeks.
Experiment 7 Reporting the Activity Date of This ADC					[115]
Related Clinical Trial
NCT Number	NCT01915472	Phase Status	Phase 2
Clinical Description	A phase 2 study of IMMU 130 (hmn-14-SN38 antibody drug conjugate) in patients with metastatic colorectal cancer.
Experiment 8 Reporting the Activity Date of This ADC					[122]
Related Clinical Trial
NCT Number	NCT01001442	Phase Status	Phase 1/2
Clinical Description	A phase 1/2a multi-dose escalation study to evaluate maximum tolerated dose (MTD), pharmacokinetics (PK), safety and efficacy of BT062 in subjects with relapsed or relapsed/refractory multiple myeloma.
Experiment 9 Reporting the Activity Date of This ADC					[125]
Patients Enrolled	Nonsmall-cell lung cancer (NSCLC) with c-Metoverexpressing tumors (c-Met positive; immunohistochemistry membrane H-score 150).
Administration Dosage	Teliso-V was administered by intravenous (IV) infusion to groups of three to six patients who were enrolled in eight-dose cohorts for dosing at 0.15 to 3.30 mg/kg on day 1, once every 21 days, or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02099058	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-399, an antibody drug conjugate, in subjects with advanced solid tumors.
Primary Endpoint	No formal MTD was identified.
Experiment 10 Reporting the Activity Date of This ADC					[126]
Related Clinical Trial
NCT Number	NCT01605318	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of once or twice weekly IMMU-130 (hMN-14-SN38, antibody-drug conjugate) in patients with colorectal cancer.
Experiment 11 Reporting the Activity Date of This ADC					[127]
Related Clinical Trial
NCT Number	NCT01270698	Phase Status	Phase 1
Clinical Description	A phase 1 study of IMMU-130 (hmn-14-SN38 antibody drug conjugate) in patients with colorectal cancer.
Experiment 12 Reporting the Activity Date of This ADC					[128]
Related Clinical Trial
NCT Number	NCT00723359	Phase Status	Phase 1
Clinical Description	A phase 1 dose escalation study to evaluate maximum tolerated dose (MTD), pharmacokinetics (PK), and safety of BT062 in subjects with relapsed or relapsed/refractory multiple myeloma.

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Objective Response Rate (ORR)	40.00% (SCCHN) 44.00% (NPC) 0.00% (CRC)
Patients Enrolled	Patients with advanced or metastatic solid tumors who had failed outcomes from or were not able to receive standard treatment were enrolled in phase 1a without EGFR prescreening. Phase 1b recruited EGFR-positive patients with refractory advanced squamous cell carcinomas of the head and neck (SCCHN), nasopharyngeal carcinoma (NPC), and colorectal cancer (CRC).    Click to Show/Hide
Administration Dosage	An intravenous dose of 0.10 to 2.50 mg/kg of MRG003 was administered every 3 weeks during phase 1a. During phase 1b, patients were administered the recommended dose identified in phase 1a.
Related Clinical Trial
NCT Number	NCT04868344	Phase Status	Phase 1
Clinical Description	An open-label, dose-finding, phase 1 study in solid tumors.
Primary Endpoint	The MRG003 recommended dose was 2.50 mg/kg.
Other Endpoint	The objective response rates for SCCHN, NPC, and CRC were 40.00%, 44.00%, and 0.00%, and the disease control rates were 100.00%, 89.00%, and 25.00%, respectively. The median DOR of all patients was 5.60 months (SCCHN: DOR, 5.60 months; 95% CI,2.80-5.60; NPC: not estimable). The median PFS of all patients was 2.80 months (95% CI,1.20-4.10 months), and the PFS of SCCHN, NPC, and CRC was 2.80 (95% CI,0.60-6.80) months, 4.00 (95% CI, 1.20-not reached) months, and 1.20 (95% CI, 0.50-2.80) months, respectively. SCCHN cohort reached the median OS as of the data cutoff date, which was 11.80 (95% CI, 3.40-11.80) months.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[116]
Related Clinical Trial
NCT Number	NCT05334810	Phase Status	Phase 2
Clinical Description	A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer.
Experiment 2 Reporting the Activity Date of This ADC					[117]
Related Clinical Trial
NCT Number	NCT04828616	Phase Status	Phase 2
Clinical Description	An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer.
Experiment 3 Reporting the Activity Date of This ADC					[118]
Related Clinical Trial
NCT Number	NCT04826107	Phase Status	Phase 2
Clinical Description	An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression.
Experiment 4 Reporting the Activity Date of This ADC					[129]
Related Clinical Trial
NCT Number	NCT04146610	Phase Status	Phase 1
Clinical Description	A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 7.60% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.20% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.47% (Day 18)	High HER2 expression (HER2+++/++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.60% (Day 25)	High HER2 expression (HER2+++/++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 39.00% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	DP303c (0.3 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.26% (Day 18)	High HER2 expression (HER2+++/++)
Method Description	DP303c (1 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.40% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 0.1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.10% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 9 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.94% (Day 18)	High HER2 expression (HER2+++/++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 10 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.48% (Day 21)	High HER2 expression (HER2+++/++)
Method Description	DP001 (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 11 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.60% (Day 25)	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 12 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 25)	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 13 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 25)	High HER2 expression (HER2+++/++)
Method Description	DP303c (2.5 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 25)	High HER2 expression (HER2+++/++)
Method Description	DP303c (5 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 15 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.10% (Day 18)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 16 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.16% (Day 18)	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 17 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.30% (Day 21)	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 18 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 21)	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 19 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 21)	High HER2 expression (HER2+++/++)
Method Description	DP303c (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 20 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 21)	High HER2 expression (HER2+++/++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 21 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.50% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 2.5 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 23 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.50% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 24 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 5 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 25 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80% (Day 18)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 26 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 27 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 28 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.54% (Day 18)	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 29 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.80% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 30 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.10% (Day 25)	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 15 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 31 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.90% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 32 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	DP303c (1 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 33 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 34 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 32)	Moderate HER2 expression (HER2++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++; HER2 MFI=157,231)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2+++; HER2 MFI=987,353)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Negative HER2 expression (HER2-; HER2 MFI=256)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2+++)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 6 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 7 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Negative HER2 expression (HER2-)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++; HER2 MFI=804,573)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++; HER2 MFI=892,333)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.39 nM	High HER2 expression (HER2+++)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 12 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.39 nM	Moderate HER2 expression (HER2++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 13 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	High HER2 expression (HER2+++; HER2 MFI=1,106,494)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 14 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 nM	High HER2 expression (HER2+++; HER2 MFI=765,629)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Partial Response (PR)	6.20%
Patients Enrolled	Advanced clear cell or papillary renal cell carcinoma (RCC) who experienced progression after at least two lines of systemic therapy, including at least one TKI were included; Additional main inclusion criteria included measurable disease by Response Criteria in Solid Tumors (RECIST) 1.1 criteria, a Karnofsky performance status 70%, and adequate renal, hepatic, and hematological laboratory values.    Click to Show/Hide
Administration Dosage	Intravenously at doses ranging from 0.15 to 2.00 mg/kg every 2 or 3 weeks until progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02837991	Phase Status	Phase 1
Clinical Description	A phase l open-label, dose escalation and cohort expansion study, to assess the safety and activity of the antibody-drug conjugate CDX-014 in advanced or metastatic renal cell carcinoma (RCC) and advanced or metastatic ovarian clear cell carcinoma (OCCC).
Primary Endpoint	One patient (6.20%) treated at 0.3 mg/kg every 3 weeks exhibited PR as best overall response,ongoing after 17 months on therapy; this patient had been on single agent PD-1 inhibition prior to initiating therapy with CDX-014. Five patients (31.00%) exhibited clinical benefit from CDX-014. PFS and OS were 2.70 months (95%CI 1.2-8.0) and 12.6 months (95%CI 5.7-12.6),respectively.    Click to Show/Hide
Other Endpoint	Partial response (PR) = 6.00% of one patient treated at 0.30 mg/kg every 3 weeks as best overall response, clinical benefit from CDX-014 of five patients = (31.25%) exhibited of at least 6 months. PFS = 2.7 months (95%CI, 1.20-8.00) ,OS =12.6 months (95%CI, 5.70-12.60).

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.00%	Positive TIM1 expression (TIM1+++/++)
Method Description	Anti-TIM-1-vcMMAE (CDX-014=300 g), CDX-014 inhibited the increase in tumor volumes relative to saline control treatment.
In Vivo Model	IGROV-1 xenograft mouse models
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 21.00%	Positive TIM1 expression (TIM1+++/++)
Method Description	Anti-TIM-1-vcMMAE (CDX-014=300 g).
In Vivo Model	A549 xenograft mouse models
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.90%	Positive TIM1 expression (TIM1+++/++)
Method Description	Anti-TIM-1-vcMMAE (CDX-014=300 g).
In Vivo Model	Caki-1 xenograft mouse model
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.50%	Positive TIM1 expression (TIM1+++/++)
Method Description	Extended dosing of CDX-014 ADC in the A549 tumor model. Three cycles of four doses of CDX-014 prolong the inhibition of tumor growth.
In Vivo Model	A549 xenograft mouse models
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Partial Response (PR)	7.69%
Patients Enrolled	Stage IIIB or IV squamous (or mixed adenosquamous) lung cancer measurable by Response Evaluation Criteria in Solid Tumors (RECIST 1.1).
Administration Dosage	A dose of 1.90 mg/kg as a 90-minute intravenous infusion for the escalation phase, on the basis of previous clinical trial results using glembatumumab vedotin at 1.3 mg/kg one-dose level; every 3 weeks.
Related Clinical Trial
NCT Number	NCT02713828	Phase Status	Phase 1
Clinical Description	A phase 1/2 study of glembatumumab vedotin in patients with gpNMB-expressing, advanced or metastatic squamous cell carcinoma of the lung.
Primary Endpoint	To further characterize the safety of this drug, the protocol was modified and additional three patients were added to cohort 1 for a total of nine patients at 1.90 mg/kg dose. A second DLT was observed in cohort 1. The patient experienced grade 3 treatment-related pruritus requiring hospital admission. The dose was de-escalated to dose level 1. No DLT was observed at dose level 1 of 1.30 mg/kg.    Click to Show/Hide
Other Endpoint	The best objective response per RECIST 1.1 was of one patient who achieved a partial response (1 of 13 [7.69%], 90% CI: 0.40%-31.60%).The median OS in this heavily pretreated population was 5.70 months (90% CI: 2.50-16.80). All patients had disease progression or died. The median PFS was 2.50 months (90% CI: 1.60-5.30).
Experiment 2 Reporting the Activity Date of This ADC					[138]
Efficacy Data	Objective Response Rate (ORR)	11.00% (all) 21.00% (patients who developed rash during the first cycle) 7.00% (those who did not)
Patients Enrolled	Stage III or IV, histologically confirmed melanoma. Patients must had previously received no more than one prior chemotherapy-containing treatment regimen for advanced disease, at least one checkpoint inhibitor (ie, antiCTLA-4, PD-1, PD-L1targeted immunotherapy), and at least one BRAF-targeted and/or MEK-targeted therapy if melanoma harbored a BRAFV600 mutation, unless it was not clinically indicated or was refused by the patient.    Click to Show/Hide
Administration Dosage	As a 90-minute intravenous infusion every 3 weeks at a starting dose of 1.90 mg/kg. Dose reductions to 1.30 and 1.00 mg/kg were allowed for toxicity.
Related Clinical Trial
NCT Number	NCT02302339	Phase Status	Phase 2
Clinical Description	A phase 2 study of glembatumumab vedotin, an anti-gpNMB antibody-drug conjugate, as monotherapy or in combination with immunotherapies in patients with advanced melanoma.
Primary Endpoint	The ORR was 11.00% and the median response duration was 6.00 months (95% confidence interval [CI],4.10 months to not reached). The median PFS was 4.40 months (95% CI,2.60-5.50 months),and the median OS was 9.00 months (95% CI,6.10-11.70 months).
Other Endpoint	For patients who developed rash during the first cycle versus those who did not,the ORR was 21.00% versus 7.00%, respectively, and there was an overall improvement in PFS (hazard ratio,0.43; P = 0.013) and OS (hazard ratio,0.43; P = 0.017).
Experiment 3 Reporting the Activity Date of This ADC					[141]
Efficacy Data	Objective Response Rate (ORR)	12.00% (for all evaluable patients treated at the phase II dose) 18.00% (evaluable patients with gpNMB-positive tumors)
Patients Enrolled	Locally advanced or metastatic carcinoma of the breast, progressive within 6 months of last therapy; received at least two prior chemotherapeutic regimens for breast cancer, with at least one given in the locally advanced or metastatic setting.
Administration Dosage	Glembatumumab vedotin was administered as a 90 minute intravenous infusion, once every 3 weeks (day 1 of repeated 21 day cycles). Delays of up to 3 weeks and up to two dose reductions (to dose levels of 1.34, 1.00, and 0.75 mg/kg, as applicable) were permitted for toxicity. Dosing continued until unmanageable treatment-related toxicities, disease progression, or death.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[142]
Related Clinical Trial
NCT Number	NCT01156753	Phase Status	Phase 2
Clinical Description	A phase 2, randomized, multicenter study of CDX-011 (CR011-vcMMAE) in patients with advanced GPNMB-expressing breast cancer.

Experiment 1 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.33% (Day 35)	High GPNMB expression (GPNMB+++)
Method Description	Tumor xenografts were generated by injecting UOK124 cells subcutaneously into flanks of athymic nude mice. Mice were randomized into treatment groups (n = 10 mice/group) based on tumor volume and treated with the following agents, singly or in combination CDX-011.
In Vivo Model	UOK124 CDX model
In Vitro Model	Papillary renal cell carcinoma	UOK124 cells		CVCL_B105

Experiment 1 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Partial Response (PR)	15.90% (all) 33.30% (FOLR1/TRPV6 high)
Patients Enrolled	Patients with platinum-resistant ovarian cancer (OC), metastatic triple negative breast cancer (TNBC) and received median 3 prior regimens.
Administration Dosage	0.15, 0.17, 0.18 mg/kg day1 and day15; q28d.
Related Clinical Trial
NCT Number	NCT04740398	Phase Status	Phase 1
Clinical Description	A phase 1a/1b, open-label, multi-center, first in human and expansion study to assess the safety, tolerance, and pharmacokinetics of the novel antitumor agent CBP-1008 in patients with advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[136]
Efficacy Data	Partial Response (PR)	20.00% (dose of 3 mg/kg) 50.00% (dose of 5 mg/kg)	High CD71 expression (CD71+++)
Patients Enrolled	Metastatic or locally advanced unresectable solid tumors without approved life-prolonging treatment options.
Administration Dosage	CX-2029 (0.10, 0.25, 0.50, 1, 2, 3, 4, or 5 mg/kg) i.v. over 90 minutes [later increased to 180 minutes to mitigate infusion-related reactions (IRR)] every 3 weeks.
Related Clinical Trial
NCT Number	NCT03543813	Phase Status	Phase 1
Clinical Description	A phase 1-2, first-in-human study of CX-2029 in adults with metastatic or locally advanced unresectable solid tumors or diffuse large B-cell lymphomas (PROCLAIM-CX-2029).
Primary Endpoint	For the dose of 3 mg/kg, confirmed partial response rate=20.00% (n=2, 95% CI=2.50-55.60). For the dose of 5 mg/kg, confirmed partial response rate=50.00% (n=1, 95% CI=1.30-98.70).
Other Endpoint	For the dose of 0.5 mg/kg, Disease controla rate=50.00% (n=3, 95% CI=11.80-82.20). For the dose of 2 mg/kg, Disease controla rate=28.60% (n=2, 95% CI=3.7-71.0). For the dose of 3 mg/kg, Disease controla rate=50.00% (n=5, 95% CI 18.70-81.30). For the dose of 5 mg/kg, Disease controla rate=50.00% (n=1, 95% CI 1.30-98.70).

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.10% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Pancreatic cancer PDX model (PDX: PA6237)
Experiment 2 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.80% (Day 18)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 9. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	CTG-820 PDX model
Experiment 3 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 4 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.00% (Day 32)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 10. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	CTG-820 PDX model
Experiment 5 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.00% (Day 18)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 13. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	CTG-820 PDX model
Experiment 6 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.40% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Gastric cancer PDX models (PDX: GA6881)
Experiment 7 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 3 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Breast cancer PDX model (PDX: CTG-0708)
Experiment 8 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Pancreatic cancer PDX model (PDX: PA6237)
Experiment 9 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Experiment 10 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: CTG-820)
Experiment 11 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Breast cancer PDX model (PDX: CTG-0708)
Experiment 12 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Gastric cancer PDX models (PDX: GA6881)
Experiment 13 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	High CD71 expression (CD71+++)
Method Description	Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS) , 6 mg/kg on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.
In Vivo Model	Esophageal caner PDX model (PDX: ES0136)
Experiment 14 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 21)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 7. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PA6237)
Experiment 15 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 18)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 8. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Diffuse large B-cell lymphoma PDX model (PDX: LY6934)
Experiment 16 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 36)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 11. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: GA6881)
Experiment 17 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 40)	High CD71 expression (CD71+++)
Method Description	Female BALB/c nude mice used for esophageal,gastric,pancreatic models,and NOD/SCID,NPG,or NOG mice used for DLBCL models and used at ages 5 to 7 weeks. Seven- to 8-week-old female Athymic Nude-Foxn1nu mice were used for breast,HNSCC,and NSCLC models (Envigo). Human cancer cell lines or tumor fragments 2 to 3 mm in diameter from stock mice inoculated with primary human tumor xenografts were harvested and used to inoculate study mice by subcutaneous injection into the right flank. When tumors reached approximately 100 to 200 mm3,mice were randomized into treatment groups based on tumor volume and body weight. Dosing started on the same day for all groups,and dosing volume was adjusted for each mouse based on body weight on day of dosing. PDX models were intravenously dosed with vehicle (PBS),1.5 mg/kg,3 mg/kg,or 6 mg anti-CD71 PDC on day 0 and day 12. Mice were checked daily for morbidity and mortality. Tumors were measured twice weekly via calipers.    Click to Show/Hide
In Vivo Model	Esophageal cancer PDX model (PDX: ES0136)

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.20 nM
Method Description	Suspension or adherent cells were plated at a density of 1, 000 cells/well in 50-mL complete media in a 96-well white-walled tissue culture plate and used immediately or allowed to adhere overnight. Cells were then incubated with 50 uL of a 2 final concentration of test article for 3 to 5 days at 37 and 5% CO2.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 2 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.30 nM	High CD71 expression (CD71+++)
Method Description	Suspension or adherent cells were plated at a density of 1, 000 cells/well in 50-mL complete media in a 96-well white-walled tissue culture plate and used immediately or allowed to adhere overnight. Cells were then incubated with 50 uL of a 2 final concentration of test article for 3 to 5 days at 37 and 5% CO2.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

Experiment 1 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Partial Response (PR)	22.20%
Patients Enrolled	Metastatic castration-resistant prostate cancer (CRPC).
Administration Dosage	Intravenous FOR46 on day 1 of every 21-day cycle. Dose levels ranged from 0.10 mg/kg. the starting dose level, to 3.00 mg/kg. The trial established 2.70 mg/kg to be the maximum tolerated dose (MTD) and the recommended phase 2 dose (RP2D) of the agent.
Related Clinical Trial
NCT Number	NCT03575819	Phase Status	Phase 1
Clinical Description	A phase 1 study of FOR46 administered every 21 days in patients with metastatic castration-resistant prostate cancer (mCRPC).
Primary Endpoint	MtD and phase 1b dose=2.70 mg/kg.
Other Endpoint	18 pts had measurable lesions; 8 of 18 (44.44%) had tumor regression, with 4 (22.22%) confirmed partial responses (PR). The median duration of response is > 14 wks (range 9 -31+ weeks).
Experiment 2 Reporting the Activity Date of This ADC					[147]
Related Clinical Trial
NCT Number	NCT05011188	Phase Status	Phase 1/2
Clinical Description	A phase 1b/2 study of FOR46 in combination with enzalutamide in patients with metastatic castration resistant prostate cancer.
Experiment 3 Reporting the Activity Date of This ADC					[152]
Related Clinical Trial
NCT Number	NCT03650491	Phase Status	Phase 1
Clinical Description	A phase 1 study of FOR46 administered every 21 days in patients with relapsed or refractory multiple myeloma (RRMM).

Experiment 1 Reporting the Activity Date of This ADC					[139]
Efficacy Data	Objective Response Rate (ORR)	35.00%
Patients Enrolled	Unresectable locally advanced or metastatic triple-negative breast cancer (mTNBC). Patients must have measureable disease per RECIST v1.1, an ECOG score of 0 or 1, and no prior cytotoxic or anti-PD-L1 treatment for advanced disease.
Administration Dosage	LV 2.50 mg/kg + pembrolizumab 200 mg intravenously every three weeks.
Related Clinical Trial
NCT Number	NCT03310957	Phase Status	Phase 1/2
Clinical Description	Single arm, open label phase 1b/2 study of SGN-LIV1A in combination with pembrolizumab for first-line treatment of patients with unresectable locally-advanced or metastatic triple-negative breast cancer.
Experiment 2 Reporting the Activity Date of This ADC					[140]
Efficacy Data	Objective Response Rate (ORR)	32.00%
Patients Enrolled	Women with LIV-1-positive, unresectable, locally advanced or metastatic breast cancer (LA/MBC).
Administration Dosage	Received a median of 3 cycles (range, 112) of SGN-LIV1A at doses of 0.50-2.80 mg/kg.
Related Clinical Trial
NCT Number	NCT01969643	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, dose-escalation study to evaluate the safety and tolerability of SGN-LIV1A in patients with metastatic breast cancer.
Experiment 3 Reporting the Activity Date of This ADC					[143]
Related Clinical Trial
NCT Number	NCT04032704	Phase Status	Phase 2
Clinical Description	Open-label phase 2 study of ladiratuzumab vedotin (LV) for unresectable locally advanced or metastatic solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.30 ng/mL
Method Description	The inhibitory activity of SGN-LIV1A against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[144]
Related Clinical Trial
NCT Number	NCT04681131	Phase Status	Phase 2
Clinical Description	A phase 2 study of BA3011 alone and in combination with PD-1 inhibitor in adult patients with metastatic non-small cell lung cancer (NSCLC) who had prior disease progression on a PD-1/L-1 inhibitor.
Experiment 2 Reporting the Activity Date of This ADC					[154]
Related Clinical Trial
NCT Number	NCT03425279	Phase Status	Phase 1
Clinical Description	A phase 1/ 2 safety and efficacy dose escalation/dose expansion study of a CAB-AXL-ADC, alone and in combination with a PD-1 inhibitor in adult patients with advanced solid tumors (phase 1) and adult and adolescent patients with advanced, refractory sarcoma (phase 2).

Experiment 1 Reporting the Activity Date of This ADC					[145]
Related Clinical Trial
NCT Number	NCT04175847	Phase Status	Phase 1/2
Clinical Description	To evaluate the safety of RC88 for injection in patients with advanced malignant solid tumors, multicenter, open, multi-cohort extension of efficacy and pharmacokinetic characteristics phase 1 /2a clinical study.
Experiment 2 Reporting the Activity Date of This ADC					[146]
Patients Enrolled	Patients with malignant pleural mesothelioma and MSLN in advanced malignant solid tumors.
Administration Dosage	Dose of 0.10, 0.50, 1.00, 1.50, 2.00 and 2.50 mg/kg.
Related Clinical Trial
NCT Number	NCT04175847	Phase Status	Phase 1/2
Clinical Description	To evaluate the safety of RC88 for injection in patients with advanced malignant solid tumors, multicenter, open, multi-cohort extension of efficacy and pharmacokinetic characteristics phase 1 /2a clinical study.
Experiment 3 Reporting the Activity Date of This ADC					[148]
Related Clinical Trial
NCT Number	NCT05508334	Phase Status	Phase 1
Clinical Description	An open-label, non-randomised, multicentre study to allow continued access to and assess the safety and tolerability of RC88 for patients with advanced solid tumours.

Experiment 1 Reporting the Activity Date of This ADC					[149]
Related Clinical Trial
NCT Number	NCT05205850	Phase Status	Phase 1
Clinical Description	An open, multi-center phase 1/2a clinical study of RC118 for injection in patients with locally advanced unresectable or metastatic malignant solid tumors with positive expression of CLAUDIN 18.2.
Experiment 2 Reporting the Activity Date of This ADC					[150]
Related Clinical Trial
NCT Number	NCT04914117	Phase Status	Phase 1
Clinical Description	Phase 1, first-in-human, multicentre, open-label study of RC118 for injection in patients with locally advanced unresectable/metastatic solid tumours.
Experiment 3 Reporting the Activity Date of This ADC					[151]
Related Clinical Trial
NCT Number	NCT03895112	Phase Status	Phase 1
Clinical Description	Phase 1 study of AVID200 in patients with myelofibrosis (myeloproliferative neoplasms research consortium [MPN-RC] 118).

Experiment 1 Reporting the Activity Date of This ADC					[153]
Patients Enrolled	Advanced solid tumors that had been previously treated with standard-of-care therapy and their physicians had determined that such therapy was no longer effective, or patients had declined to receive further standard-of-care treatments.
Administration Dosage	The starting dose of 0.40 mg/kg on day 1 of each 21-day cycle; A standard 3 + 3 dose-escalation design was used, and doses of 0.80, 1.20, and 1.60 mg/kg were also administered on day 1 of each 21-day cycle; intravenous infusion over 60 minutes.
Related Clinical Trial
NCT Number	NCT04084366	Phase Status	Phase 1
Clinical Description	A phase 1/2, open-label, dose-escalation and cohort-expansion study evaluating the safety, pharmacokinetics, and therapeutic activity of OBI-999 in patients with advanced solid tumors.
Primary Endpoint	The incidence of dose-limiting toxicities and adverse events and determination of the maximum tolerated dose (MTD)/recommended phase II dose.

Experiment 1 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.00% (Day 26)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 0.3 mg/kg, qw*6.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.00% (Day 77)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 1 mg/kg, qw*6.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.00% (Day 53)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 1 mg/kg, qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.00% (Day 25)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 5 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.00% (Day 77)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*2.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 53)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 53)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 1-3 mg/kg, qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.00% (Day 77)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 3 mg/kg, qw*6.
In Vivo Model	MCF-7 CDX model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 37)	Positive Globo H expression (Globo H+++/++)
Method Description	Mice were treated with an intravenous dose of the ADCs at 10 mg/kg, qw*4.
In Vivo Model	HPAC CDX model
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.70%
Method Description	In vivo , In each animal study,the antitumor efficacy was evaluated with doses of 1.00, 3.00, or 10.00 mg/kg of OBI-999 via i.v. injection. In NCI-N87 xenograft model,treatment groups of MMAE 0.191 mg/kg and Ctrl-ADC 3 mg/kg were also included. Each study utilized 6 to 8 mice per group.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
	Breast adenocarcinoma	HCC1428 cells		CVCL_1252

Experiment 1 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFE772; EGFR mutation)
Experiment 2 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 6.00% (Day 25)	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in Nonresponder.
In Vivo Model	NSCLC PDX model
Experiment 3 Reporting the Activity Date of This ADC					[156]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.30% (Day 21)	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). Enapotamab vedotin and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 4 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.50% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU2511; EGFR mutation)
Experiment 5 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.50% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0858; EGFR L858R mutation)
Experiment 6 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	29.60% (Day 49)	Positive AXL expression (AXL+++/++)
Method Description	EnaV=2 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395)
Experiment 7 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	46.90% (Day 49)	Positive AXL expression (AXL+++/++)
Method Description	EnaV=4 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395)
Experiment 8 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.00% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA677; EGFR mutation)
Experiment 9 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.00% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU1868; EGFR L858R and T790Mmutations)
Experiment 10 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.00% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LCx-MR007; Osimertinib resistant)
Experiment 11 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.40% (Day 15)	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in intermediate.
In Vivo Model	NSCLC PDX model
Experiment 12 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	60.00% (Day 10)	Moderate AXL expression (AXL++; IHC H-score=121)
Method Description	EnaV=4 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU2511)
Experiment 13 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50% (Day 35)	Moderate AXL expression (AXL++; IHC H-score=101)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 14 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.00% (Day 35)	High AXL expression (AXL+++; IHC H-score=248)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395; EGFR mutation)
Experiment 15 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.70% (Day 23)	Moderate AXL expression (AXL++; IHC H-score=142)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas ,esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 16 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.10% (Day 14)	Moderate AXL expression (AXL++; IHC H-score=141)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 17 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.80% (Day 32)	Moderate AXL expression (AXL++; IHC H-score=183)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
In Vivo Model	Cervical cancer PDX model (PDX: CV1664)
Experiment 18 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.40% (Day 32)	Moderate AXL expression (AXL++; IHC H-score=104)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
In Vivo Model	Cervical cancer PDX model (PDX: CV1664)
Experiment 19 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.30% (Day 14)	Negative AXL expression (AXL-; IHC H-score=0)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 20 Reporting the Activity Date of This ADC					[156]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.30% (Day 21)	High AXL expression (AXL+++; IHC H-score=305)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (4 mg/kg,q.d.). Enapotamab vedotin and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 21 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80% (Day 23)	Moderate AXL expression (AXL++; IHC H-score=117)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 22 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA677_R, EGFRi resistant)
Experiment 23 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 30)	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in responder.
In Vivo Model	NSCLC PDX model
Experiment 24 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	70.55 ng/mL	Moderate AXL expression (AXL++; 22,304 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vivo Model	Melanoma PDX model (PDX: M019R.X1.CL)
In Vitro Model	Melanoma	M019R.X1.CL cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.00% (Day 34)	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 2 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.70% (Day 28)	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells + Ctrl ADC.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 3 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	34.30% (Day 10)	Positive AXL expression (AXL+++/++)
Method Description	EnaV=2 mg/kg.
In Vivo Model	LU2511 in NSCLC CDX model
Experiment 4 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	40.90% (Day 21)	Positive AXL expression (AXL+++/++)
Method Description	EnaV=0.5 mg/kg.
In Vivo Model	LCLC-103H in NSCLC CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 5 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.40% (Day 34)	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
In Vivo Model	LCLC-103H xenograft model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 6 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.00% (Day 28)	Positive AXL expression (AXL+++/++)
Method Description	Treated with Ctrl T cells + EnaV.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 7 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.70% (Day 22)	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
In Vivo Model	BLM cell line xenograft model
In Vitro Model	Amelanotic melanoma	BLM cells		CVCL_7035
Experiment 8 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50% (Day 35)	Positive AXL expression (AXL+++/++)
In Vivo Model	LCLC-103H CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 9 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50% (Day 10)	Positive AXL expression (AXL+++/++)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
In Vivo Model	Melanoma CDX model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 10 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.20% (Day 28)	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells + EnaV.
In Vivo Model	SkMel-147 cell line xenograft model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 11 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.70% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 12 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.60% (Day 10)	Positive AXL expression (AXL+++/++)
Method Description	The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
In Vivo Model	Melanoma CDX model
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 13 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.80% (Day 21)	Positive AXL expression (AXL+++/++)
Method Description	EnaV=1 mg/kg.
In Vivo Model	LCLC-103H in NSCLC CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM±0.016 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM±0.005 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM±0.005 nM	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 4 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 5 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 6 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 7 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.50 ng/mL	Moderate AXL expression (AXL++; 37,235 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	A-875 cells		CVCL_4733
Experiment 8 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.34 ng/mL	Moderate AXL expression (AXL++; 54,946 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells (BRAF inhibitor resistant)		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.70 ng/mL	High AXL expression (AXL+++; 117,665 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 10 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.30 ng/mL	Moderate AXL expression (AXL++; 46,701 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	42.06 ng/mL	Moderate AXL expression (AXL++; 35,452 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 12 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.54 ng/mL	High AXL expression (AXL+++; 169,192 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 13 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	189.30 ng/mL	Moderate AXL expression (AXL++; 70,222 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	SK-MEL-2 cells (MEK inhibitor-resistant)		CVCL_0069
Experiment 14 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	190.90 ng/mL	Moderate AXL expression (AXL++; 83,986 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 15 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	370.40 ng/mL	Moderate AXL expression (AXL++; 16,611 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Amelanotic melanoma	A375/R cells		CVCL_IW10
Experiment 16 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	887.20 ng/mL	Moderate AXL expression (AXL++; 16,611 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vivo Model	Melanoma PDX model (PDX: M016.X1.CL)
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 17 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1828.30 ng/mL	Moderate AXL expression (AXL++; 66,691 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 18 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2090.30 ng/mL	Moderate AXL expression (AXL++; 34,978 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 19 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2895.70 ng/mL	Moderate AXL expression (AXL++; 28,000 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 20 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6881.00 ng/mL	Low AXL expression (AXL+; 9,138 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 21 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative AXL expression (AXL-; 528 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 22 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Moderate AXL expression (AXL++; 37,506 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 23 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Low AXL expression (AXL+; 2,326 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 24 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative AXL expression (AXL-; 150 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 25 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative AXL expression (AXL-; 250 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 26 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative AXL expression (AXL-; 325 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 27 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative AXL expression (AXL-; 100 AXL receptor copy number)
Method Description	All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
In Vitro Model	Melanoma	SK-MEL-2 cells		CVCL_0069
Experiment 28 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.195±0.068	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00%	High GPRC5D expression (GPRC5D+++)
Method Description	The inhibitory activity of LM-305 against cancer cell growth was evaluated in Multiple myeloma CDX model in vivo. The dose of LM-305 was 3 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Multiple myeloma	Multiple myeloma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10-0.30 nM	High GPRC5D expression (GPRC5D+++)
Method Description	LM-305 was evaluated in vitro for its cytotoxic activity against a panel of multiple myeloma cell lines. LM-305 was co-cultured with multiple myeloma cells.
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10-0.30 nM	High GPRC5D expression (GPRC5D+++)
Method Description	LM-305 was evaluated in vitro for its cytotoxic activity against a panel of multiple myeloma cell lines. LM-305 was co-cultured with multiple myeloma cells.
In Vitro Model	Plasma cell myeloma	MM1.R cells		CVCL_8794

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Objective Response Rate (ORR)	2.10% (non-sarcomas all doses) 10.80% (sarcomas all dose) 20.00% (osteosarcoma+UPS 3.6 mg/kg) 20.00% (osteosarcoma 3.6 mg/kg) 20.00% (UPS 3.6 mg/kg)
Patients Enrolled	Patients with LRRC15 positive squamous cell carcinoma of the head and neck, NSCKC, breast cancer, undifferentiated pleomorphic sarcoma or osteosarcoma.
Administration Dosage	0.30 up to 6.00 mg/kg on day 1, once every 2 weeks.
Related Clinical Trial
NCT Number	NCT02565758	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1, open-label, dose-escalation study of ABBV-085, an antibody drug conjugate, in subjects with advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[180]
Related Clinical Trial
NCT Number	NCT02565758	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1, open-label, dose-escalation study of ABBV-085, an antibody drug conjugate, in subjects with advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.90% (Day 20)	Negative LRRC15 (LRRC15-)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Liposarcoma PDX model (PDX: LPS28)
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.50% (Day 22)	Negative LRRC15 (LRRC15-)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma PDX model (PDX: LMS33)
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.10% (Day 43)	Negative LRRC15 (LRRC15-)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Liposarcoma PDX model (PDX: LPS28)
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.20% (Day 20)	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Liposarcoma PDX model (PDX: LPS28)
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.70% (Day 25)	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma PDX model (PDX: LMS33)
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.20% (Day 21)	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma and undifferentiated sarcomas PDX model, (PDX: UPS7)
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 22)	High LRRC15 expression (LRRC15+++)
Method Description	The efficacy of ABBV-085 directed against LRRC15 was assessed in several patient-derived xenograft models of UPS,LMS,and DDLPS. For efficacy study,tumors were allowed to establish to 200±50 mm3 in size before randomization into various treatment groups with 7-9 mice per group. Isotype-control,isotype-MMAE,and ABBV-085,diluted in PBS were administered at 6 mg/kg once every 4 days intraperitoneally for a total of six injections.    Click to Show/Hide
In Vivo Model	Leiomyosarcoma and undifferentiated sarcomas PDX model, (PDX: UPS7)

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Objective Response Rate (ORR)	13.00% (0.50 mg/kg) 29.00% (0.75 mg/kg) 40.00% (1.00 mg/kg) 40.00% (1.25 mg/kg)	High SLITRK6 expression (SLITRK6+++; IHC H-score=230)
Patients Enrolled	Metastatic uroepithelial carcinoma (mUC) patients unselected for SLITRK6 expression (determined by an IHC assay) and previously treated with 1 prior chemo regimen or unfit for cisplatin.
Administration Dosage	Administered IV weekly for 3 out of every 4 weeks.
Related Clinical Trial
NCT Number	NCT01963052	Phase Status	Phase 1
Clinical Description	A phase 1 study of the safety and pharmacokinetics of escalating doses of AGS15E given as monotherapy in subjects with metastatic urothelial cancer.

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.40% (Day 17)	Moderate SLITRK6 expression (SLITRK6++; IHC H-score=185)
Method Description	PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,Sirtratumab Vedotin was dosed at 0.25 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B8)
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.90% (Day 25)	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,Sirtratumab Vedotin was dosed at 0.5 mg/kg,2x per week i.v in AG-B7 PDX model. The last dose was given on day 21.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B7)
Experiment 3 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.40% (Day 17)	High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description	PDX models were established by subcutaneous implantation of xenograft fragments (AG-B7 or AG-B8) in the flanks of SCID mice. When the tumor volume reached approximately 200 mm3,Sirtratumab Vedotin was dosed at 0.5 mg/kg,2x per week i.v in AG-B8 PDX model. The last dose was given on day 14.
In Vivo Model	Bladder cancer PDX model (PDX: AG-B8)

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.90% (Day 30)	High SLITRK6 expression (SLITRK6+++)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Sirtratumab Vedotin, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder carcinoma	RT-4 cells		CVCL_0036
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.10% (Day 21)	Negative SLITRK6 expression (SLITRK6-)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. Sirtratumab Vedotin was administered twice weekly at 3 mg/kg (n = 6) starting when the tumor volume reached approximately 200 mm3.
In Vivo Model	Lung cancer NCI-322M CDX model
In Vitro Model	Lung cancer	NCI-322M cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.99 nM
Method Description	ASG-15ME was tested for its ability to kill several SLITRK6-positive cell lines in vitro. The viability of CHP-212 cells treated with ASG-15ME was compared with that of target negative cells (IGR-OV1) or cells treated with an isotype control antibody to determine IC50 values.
In Vitro Model	Neuroblastoma	CHP-212 cells		CVCL_1125
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High SLITRK6 expression (SLITRK6+++; IHC H-score=250)
Method Description	ASG-15ME was tested for its ability to kill several SLITRK6-positive cell lines in vitro. The viability of CHP-212 cells treated with ASG-15ME was compared with that of target negative cells (IGR-OV1) or cells treated with an isotype control antibody to determine IC50 values.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[169]
Efficacy Data	Objective Response Rate (ORR)	17.76%
Patients Enrolled	Eastern Cooperative Oncology Group (ECOG) performance status of 0-1, histologically or cytologically documented advanced or metastatic breast, ovarian, pancreatic, NSCLC, head and neck squamous cell carcinoma, or gastric cancer in dose escalation, adequate hematologic and end organ function, and measurable disease per RECIST v1.1.
Administration Dosage	Intravenously at doses of 0.20, 0.40, 0.80, 1.60, or 2.40 mg/kg once every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT02092792	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study evaluating the safety and tolerability of escalating doses of DLYE5953A in patients with refractory solid tumors.
Primary Endpoint	The confirmed overall objective response rate was 17.76%. All responders (8/68 patients) had PR,and all had received the RP2D dose of 2.40 mg/kg. This included three patients with MBC, and five patients in the NSCLC expansion cohort (5/25; 20%).
Other Endpoint	The recommended phase II dose (RP2D) was 2.40 mg/kg Q3W. No dose-limiting toxicities were identified during dose escalation (0.20-2.40 mg/kg; n = 20).

Experiment 1 Reporting the Activity Date of This ADC					[170]
Efficacy Data	Objective Response Rate (ORR)	23.81% (among 21 pts who had at least one tumor assessment) 33.33% (in the 1.8 mg/kg cohort, DLBCL) 66.7% ( in the 2.5 mg/kg cohort, FL)
Patients Enrolled	CD20-positive relapsed or refractory (R/R) B-cell non Hodgkin lymphoma (NHL).
Administration Dosage	Six dose levels ranging from 0.15 to 2.50 mg/kg, intravenously once every 3 weeks (Q3W) for a maximum of 6 treatment cycles.
Related Clinical Trial
NCT Number	NCT05155839	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, first-in-human, phase 1 dose-escalation and expansion clinical study to assess the safety, tolerability, pharmacokinetics and preliminary efficacy of MRG001 in patients with CD20-positive relapsed or refractory B-cell non-Hodgkin lymphoma (NHL).
Primary Endpoint	Rp2D=1.80 mg/kg.
Other Endpoint	Among 21 pts who had at least one tumor assessment, ORR=23.81% , PR rate=19.05% (N=4),CR rate=4.76% (N=1).
Experiment 2 Reporting the Activity Date of This ADC					[174]
Related Clinical Trial
NCT Number	NCT05844527	Phase Status	Phase 2
Clinical Description	Safety and efficacy of MRG-001 in wound healing in pre-abdominoplasty surgical excisions and scar appearance in subjects undergoing abdominoplasty.

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Objective Response Rate (ORR)	24.00% (0.9 1.2 and 1.5 mg/kg)	Low CD37 expression (CD37+; CD37 MFI ratio=82)
Patients Enrolled	Relapsed / refractory non Hodgkin lymphomas (NHLs) and chronic lymphocytic leukemia (CLL).
Administration Dosage	Administered intravenously (IV) once every 3 weeks (Q3 weeks) until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02175433	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with refractory or relapsed lymphoid malignancies.
Experiment 2 Reporting the Activity Date of This ADC					[182]
Related Clinical Trial
NCT Number	NCT02610062	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating safety, tolerability, and pharmacokinetics of escalating doses of AGS67E given as monotherapy in subjects with acute myeloid leukemia (AML).

Experiment 1 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0.00%	Low CD37 expression (CD37+; CD37 MFI ratio=82)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Hel 92.1.7 AmL cancer xenograft model
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	27.00%	High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 3 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	31.00%	High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing WSU-DLCL2 DBCL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 4 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	41.00%	Low CD37 expression (CD37+; CD37 MFI ratio=20)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing KG-1 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 5 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	51.00%	High CD37 expression (CD37+++; CD37 MFI ratio=300)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Mino MCL cancer xenograft model
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 6 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	63.00%	Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 7 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	66.00%	High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 8 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	69.00%	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 9 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	86.00%	Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 10 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.00%	High CD37 expression (CD37+++; CD37 MFI ratio=300)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Mino MCL cancer xenograft model
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 11 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95.00%	High CD37 expression (CD37+++; CD37 MFI ratio=580)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing DOHH2 FL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 12 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95.00%	Low CD37 expression (CD37+; CD37 MFI ratio=23)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing THP-1 AmL cancer xenograft models
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 13 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.00%	High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing WSU-DLCL2 DBCL cancer xenograft model
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 14 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	97.00%	Moderate CD37 expression (CD37++; CD37 MFI ratio=140)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing Ramos-RR-XcL Burkitt lymphoma cancer xenograft model
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 15 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 16 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 17 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing JVM3 xenograft CLL cancer model
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 18 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 19 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 20 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD38-expressing MV-411 AmL cancer xenograft model
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 21 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 22 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The in vivo antitumor activity of AGS-67E was evaluated in a CD37 positive NHL,CLL and AmL cell line xenograft models. Depending on the cell line,110e6 cells were injected into the flanks of individual SCID mice,and tumor volumes were allowed to reach 100 to 300 mm3. Animals and their tumors were size matched and randomized into treatment and control groups. Depending on the study,AGS67E and an isotype control ADC were dosed by i.v. bolus injection either at 0.25,0.75,1.5,or 3.0 mg/kg at biweekly (BIW) or weekly (QW) frequencies and for a total of 2 to 4 doses.    Click to Show/Hide
In Vivo Model	CD37-expressing MOLM-13 AmL cancer xenograft model
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119

Experiment 1 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05±0.03 nM	Low CD37 expression (CD37+; CD37 MFI ratio=25)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07±0.49 nM	Low CD37 expression (CD37+; CD37 MFI ratio=18)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 3 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.02 nM
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 4 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.61 nM	Negative CD37 expression (CD37-; CD37 MFI ratio=3)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	Granta-519 cells		CVCL_1818
Experiment 5 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13±0.08 nM	High CD37 expression (CD37+++; CD37 MFI ratio=662)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 6 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23±0.30 nM	High CD37 expression (CD37+++; CD37 MFI ratio=534)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma	SU-DHL-4 cells		CVCL_0539
Experiment 7 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50±0.72 nM	High CD37 expression (CD37+++; CD37 MFI ratio=581)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	B-cell prolymphocytic leukemia	JVM-3 cells		CVCL_1320
Experiment 8 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.71±0.20 nM	Low CD37 expression (CD37+; CD37 MFI ratio=22)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	SKM-1 cells		CVCL_0098
Experiment 9 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.98±1.10 nM	Negative CD37 expression (CD37-; CD37 MFI ratio=9)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 10 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.10±0.60 nM	Moderate CD37 expression (CD37++; CD37 MFI ratio=129)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	OCI-AML-2 cells		CVCL_1619
Experiment 11 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.20±0.90 nM	Negative CD37 expression (CD37-; CD37 MFI ratio=1)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 12 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.30±0.50 nM	Low CD37 expression (CD37+; CD37 MFI ratio=20)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	MOLM-13 cells		CVCL_2119
Experiment 13 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.50±0.70 nM	Low CD37 expression (CD37+; CD37 MFI ratio=11)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.70±1.60 nM	Low CD37 expression (CD37+; CD37 MFI ratio=26)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	BDCM cells		CVCL_4613
Experiment 15 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.70±3.00 nM	High CD37 expression (CD37+++; CD37 MFI ratio=341)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma	WSU-DLCL2 cells		CVCL_1902
Experiment 16 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High CD37 expression (CD37+++; CD37 MFI ratio=301)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	REC-1 cells		CVCL_1884
Experiment 17 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High CD37 expression (CD37+++; CD37 MFI ratio=554)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	PL-21 cells		CVCL_2161
Experiment 18 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Low CD37 expression (CD37+; CD37 MFI ratio=39)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 19 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	High CD37 expression (CD37+++; CD37 MFI ratio=372)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 20 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Negative CD37 expression (CD37-; CD37 MFI ratio=4)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute megakaryoblastic leukemia	UT-7 cells		CVCL_2233
Experiment 21 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Negative CD37 expression (CD37-; CD37 MFI ratio=5)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 22 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Low CD37 expression (CD37+; CD37 MFI ratio=30)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Down syndrome	CMK cells		CVCL_0216
Experiment 23 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Low CD37 expression (CD37+; CD37 MFI ratio=10)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute erythroid leukemia	TF-1a cells		CVCL_3608
Experiment 24 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Low CD37 expression (CD37+; CD37 MFI ratio=64)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Acute erythroid leukemia	HEL 92.1 cells		CVCL_2481
Experiment 25 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Low CD37 expression (CD37+; CD37 MFI ratio=23)
Method Description	The inhibitory activity of AGS-67E against cancer cell growth was evaluated in various human cancer cell lines in vitro. Exponentially growing cells with a viability of 95% or greater were plated in fresh RPMI-1640 (Gibco-Invitrogen) media containing phenol red supplemented with 10% FBS (heat inactivated),10 mmol/L Hepes,and 1 mmol/L sodium pyruvate. Cells were left overnight and treated with AGS67E and an isotype control. After 5 days of treatment and incubation at 37°C and 5% CO2,cell viability was measured following a 1 hour incubation at 37°C with Presto Blue Reagent (Invitrogen).    Click to Show/Hide
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Objective Response Rate (ORR)	46.67%
Patients Enrolled	B-non Hodgkin lymphoma (NHL) that had relapsed after or failed to respond to at least one prior treatment regimen and for which no suitable therapy of curative intent or higher priority existed.
Administration Dosage	The phase Ia, starting dose of 0.30 mg/kg administered intravenously once every 3 weeks (Q3W; 1 cycle = 21 days); The phase Ib portion evaluated DCDS0780A in dose-escalation cohorts starting at one dose level below that tolerated by completed monotherapy cohorts, and in combination with a fixed dose of rituximab (375 mg/m2); up to approximately 1 year or until disease progression or unacceptable toxicity.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02453087	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, phase 1/1b dose escalation study evaluating the pharmacokinetics, safety, tolerability, and preliminary efficacy of DCDS0780A, alone or in combination with rituximab, or obinutuzumab, in patients with relapsed/refractory B-cell non-Hodgkin's lymphoma.
Primary Endpoint	Response rate in all-treated patients (N=60) was 46.67% (n=28), including 17 complete responses (28.33%) and 11 partial responses (18.33%). The median duration of response (15.20 months) was the same for all responders (n=28) and patients with DLBCL (n=20).
Other Endpoint	The median PFS for all patients on study (N =60) was 4.40 months [95% CI,2.60-13.20], and 3.90 months (95% CI,2.40-9.50) for patients with DLBCL (n=41); PFS for pooled subgroups are indicated. The median DoR for the 28 responders among all patients was 15.20 months (95% CI,8.40-N.E.).

Experiment 1 Reporting the Activity Date of This ADC					[173]
Efficacy Data	Objective Response Rate (ORR)	47.10% (gastric cancer) 33.30% (1.00 mg/kg) 40.00% (2.00 mg/kg) 100.00% (2.50 mg/kg) 20.00% (3.00 mg/kg) 38.10% (all)
Patients Enrolled	Patients with resistant/refractory solid tumors that express CLDN18.2 who progressed on or were intolerant to standard treatment, or had no standard treatment were recruited.. ECOG score of 0-2.
Administration Dosage	0.50 up to 3.00 mg/kg on day 1, administered once every 3 weeks.
Related Clinical Trial
NCT Number	NCT05009966	Phase Status	Phase 1
Clinical Description	A phase 1 trial to evaluate safety, tolerability, pharmacokinetics, immunogenicity and initial efficacy of SYSA1801 in the treatment of CLDN 18.2 positive advanced malignant solid tumor.

Experiment 1 Reporting the Activity Date of This ADC					[175]
Patients Enrolled	Patients with metastatic or unresectable solid tumors.
Administration Dosage	30 patients in Q1W (0.80, 1.00, and 1.20 mg/kg); 18 patients in 2Q3W (1.20 or 1.25 mg/kg).
Related Clinical Trial
NCT Number	NCT04389632	Phase Status	Phase 1/2
Clinical Description	A phase 1 study of SGN-B6A in advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[176]
Related Clinical Trial
NCT Number	NCT05208762	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-PDL1V in advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[177]
Related Clinical Trial
NCT Number	NCT03379584	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-CD48A in patients with relapsed or refractory multiple myeloma.

Experiment 1 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75.00%	Positive SLAMF2 expression (SLAMF2+++/++)
Method Description	SGN-CD48A was evaluated in vivo for antitumor activity in a diffuse MM cell line xenograft model in mice. SGN-CD48A was administered at a single dose of 0.30 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Plasma cell myeloma	EJM cells		CVCL_2030
Experiment 2 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Tumor Growth Inhibition value (TGI)	87.50%	Positive SLAMF2 expression (SLAMF2+++/++)
Method Description	SGN-CD48A was evaluated in vivo for antitumor activity in a diffuse MM cell line xenograft model in mice. SGN-CD48A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Plasma cell myeloma	U-266 cells		CVCL_0015
Experiment 3 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Positive SLAMF2 expression (SLAMF2+++/++)
Method Description	SGN-CD48A was evaluated in vivo for antitumor activity in a diffuse MM cell line xenograft model in mice. SGN-CD48A was administered at a single dose of 0.30 mg/kg.
In Vivo Model	Multiple myeloma CDX model
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.00-11.00 ng/mL	High CD48 expresion (CD48+++/++; 1260 MSLN molecules/cell)
Method Description	Cytotoxic activity of SGN-CD48A was demonstrated in a panel of human MM cell lines in vitro.
In Vitro Model	Multiple myeloma	Multiple myeloma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[178]
Related Clinical Trial
NCT Number	NCT04042480	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-CD228A in select advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75.00%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 3.00 mg/kg.
In Vivo Model	NSCLC PDX model
Experiment 2 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	NSCLC PDX model

Experiment 1 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	50.00%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Melanoma CDX model
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 2 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	62.50%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Melanoma CDX model
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 3 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Positive CD228 expression (CD228+++/++)
Method Description	SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
In Vivo Model	Squamous NSCLC CDX model
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608

Experiment 1 Reporting the Activity Date of This ADC					[179]
Patients Enrolled	Locally advanced unresectable or metastatic solid tumors.
Related Clinical Trial
NCT Number	NCT05194072	Phase Status	Phase 1
Clinical Description	A phase 1 study of SGN-B7H4V in advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[181]
Patients Enrolled	Patients with advanced solid tumor types typically associated with elevated levels of EGFR expression (e.g., head and neck squamous cell carcinoma [HNC], non-small cell lung cancer [NSCLC], triple-negative breast cancer, colorectal carcinoma, and GBM.
Administration Dosage	A standard 3+3 design; intravenous (IV) infusion to groups of 3 to 6 patients. An every-3-week dosing cycle (0.30, 0.45, 0.67, 1.00, 1.50, 2.00, or 2.25 mg/kg losatuxizumab vedotin every 3 weeks [Q3W]) or alternative dosing schedules were evaluated (2.00 or 3.00 mg/kg losatuxizumab vedotin for 2 weeks on, 1 week off, or 4.50 or 6.00 mg/kg losatuxizumab vedotin weekly [over 3 weeks total]).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT02365662	Phase Status	Phase 1
Clinical Description	A phase 1 study of ABBV-221 in subjects with advanced solid tumor types likely to exhibit elevated levels of epidermal growth factor receptor.
Primary Endpoint	The maximum tolerated dose (MTD) was not achieved.
Other Endpoint	Stable disease (SD) for at least 2 cycles was observed in 19 patients (42.20%).

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Tumor Growth Inhibition value (TGI)	94.90% (Day 49)	High HER2 expression (HER2+++)
Method Description	In vivo therapy studies were conducted in mesothelioma xenograft and patient-derived xenograft (PDX) tumor model.ABT-414 treatment 3 mg/kg q4 days.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: MSTO-211H)
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.30% (Day 49)	High HER2 expression (HER2+++)
Method Description	In vivo therapy studies were conducted in mesothelioma xenograft and patient-derived xenograft (PDX) tumor model.ABBV-221 treatment 3 mg/kg q4 days.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: MSTO-211H)

Experiment 1 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.23% (Day 120)	Low EGFR expression (EGFR+)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 6 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	NCI-H292 lung xenograft tumor model
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.45% (Day 95)	Low EGFR expression (EGFR+)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 3 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	NCI-H441 lung xenograft tumor model
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.60% (Day 113)	High EGFR expression (EGFR+++)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 4 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	EBC1 lung xenograft tumor model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 4 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 113)	High EGFR expression (EGFR+++)
Method Description	To generate xenografts, a suspension of viable tumors cells mixed with an equal amount of Matrigel was injected subcutaneously into the flank of 6- to 8-week old mice. The injection volume was 0.2 mL composed of a 1:1 mixture of S-MEM and Matrigel. Tumors were size matched at approximately 200-250 mm3. Treatments ABBV-221 at 1 mg/kg every 4th day by intraperitoneal injection.    Click to Show/Hide
In Vivo Model	NCI-H1703 lung xenograft tumor model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.80% (Day 40)	Positive EGFR expression (EGFR+++/++)
Method Description	To establish xenografts, 2 x 106 MSTO-211H cells mixed with 75-uL Matrigel were injected subcutaneously in the right flank of 5 to 6-week-old female BALB/c nu/nu miceFor the MSTO-211H study, mice received either ABT-414, ABBV-221 or ADC control (3 mg/kg) every 4 days.
In Vivo Model	MSTO-211H CDX model
In Vitro Model	Pleural biphasic mesothelioma	MSTO-211H cells		CVCL_1430
Experiment 2 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Glioblastoma	U87MGde2-7 cells (EGFRvIII overexpression)		CVCL_0022
Experiment 3 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 5 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 6 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 7 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 nM	High EGFR expression (EGFR+++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827ER cells		CVCL_V408
Experiment 8 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	69.00 nM	Moderate EGFR expression (EGFR++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 9 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.00 nM	Moderate EGFR expression (EGFR++)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 10 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 nM	Low EGFR expression (EGFR+)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HCT 15 cells		CVCL_0292
Experiment 11 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 nM	Low EGFR expression (EGFR+)
Method Description	Cells were plated at 1,000 to 3,000 cells/well in complete growth medium containing 10% FBS in 96-well plates. The following day medium was removed and replaced with fresh media containing titrations of antibodies or ADCs, and cells were incubated for 72 hours at 37°C in a humidified CO2 incubator. Cell viability was then assessed using an ATPlite luminescence assay.Cell viability was determined following incubation with ABBV-221 for 72 hours.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.60 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.50 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.20 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 4 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.10 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.40 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.40 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.20 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.50 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538

Experiment 1 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive FZD7 expression (FZD7+++/++)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells (FZD7 overexpression)		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive FZD7 expression (FZD7+++/++)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian cystadenocarcinoma	MA148 cells		CVCL_AK47
Experiment 3 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive FZD7 expression (FZD7+++/++)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.00 nM	Negative FZD7 expression (FZD7-)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 5 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60.00 nM	Negative FZD7 expression (FZD7-)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian cystadenocarcinoma	MA148 cells (FZD7 knock-out)		CVCL_AK47

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.13% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: GA0045)

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.53% (Day 70)	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (1 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian cancer PDX model (PDX: Ovx6)
Experiment 2 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.47% (Day 70)	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (3 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian cancer PDX model (PDX: Ovx6)
Experiment 3 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.50% (Day 21)	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	To assess the efficacy of LSR-ADC against omental/bowel metastasis,OVCAR3-Luc xenograft models were used. The OVCAR3-Luc xenograft models was established by implanting OVCAR3-Luc cells intraperitoneally,into the subscapular areas. Six or seven weeks after the inoculation,the treatment was initiated. PBS and 10 mg/kg of LSR-ADC were intravenously injected twice a week,for a total of four times.    Click to Show/Hide
In Vivo Model	Ovarian high-grade serous carcinoma PDX model (PDX: OVCAR3-LUC)
Experiment 4 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.24% (Day 70)	High LSR expression (LSR+++; 86,697.7 LSR expression (ABC/cell))
Method Description	The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (10 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian cancer PDX model (PDX: Ovx6)

Experiment 1 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 21.41% (Day 28)	High LSR expression (LSR+++)
Method Description	The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (1 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian high-grade serous carcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.43% (Day 28)	High LSR expression (LSR+++)
Method Description	The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (3 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian high-grade serous carcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.01% (Day 28)	High LSR expression (LSR+++)
Method Description	The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (10 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian high-grade serous carcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	449.00 pM	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	High LSR expression (LSR+++; 86,697.7 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 Luc cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.74 nM	High LSR expression (LSR+++; 84,008.8 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ovarian cancer ascites	NOVC-7C cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Moderate LSR expression (LSR++; 2,631.9 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ewing sarcoma	ES2 cells		CVCL_AX39

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.70% (Day 14)	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 2 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.30% (Day 14)	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.20% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.30% (Day 67)	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established PDX model of pancreatic cancer cell implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	Pancreatic cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	501 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.00% (Day 67)	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established PDX model of pancreatic cancer cell implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	Pancreatic cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.51 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	71.00% (Day 46)	Moderate Tissue factor expression (TF++; IHC H-score=155)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 190 mm3 The model dosed weekly at 25 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) ovarian carcinomamodel
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 60)	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 210 mm3 The model dosed weekly at 5 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived head and neck carcinoma xenograft (PDX) model
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 46)	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 140 mm3 The model dosed weekly at 4 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived gastric adenocarcinoma xenograft (PDX) model

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	67.00% (Day 49)	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.00% (Day 49)	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 59)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 5 mg/kg for 3 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 5 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 nM	High Tissue factor expression (TF+++; IHC H-score=250)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 nM	High Tissue factor expression (TF+++; IHC H-score=250)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (25A-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.30% (Day 14)	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 2 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.20% (Day 14)	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.10% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	74.00% (Day 46)	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 190 mm3 The model dosed weekly at 25 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) ovarian carcinomamodel
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 60)	Low FOLR1 expression (FOLR1+)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 210 mm3 The model dosed weekly at 5 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) head and neck carcinoma model

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	48.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 59)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 5 mg/kg for 3 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 5 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	43.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (43Ea-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.49% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (1.1 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: LU2535)
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: GA0045)
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3.3 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: LU2535)
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: LU2535)

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (0.75 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (1.5 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 21)	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[195]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80% (Day 35)	High GPC1 expression (GPC1+++)
In Vivo Model	Pancreatic cancer PDX model (PDX: PK645)
Experiment 2 Reporting the Activity Date of This ADC					[195]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70% (Day 28)	High GPC1 expression (GPC1+++)
In Vivo Model	Pancreatic cancer PDX model (PDX: PK565)

Experiment 1 Reporting the Activity Date of This ADC					[195]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.90 pM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic carcinoma	KP-2 cells		CVCL_3004
Experiment 2 Reporting the Activity Date of This ADC					[195]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 nM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic ductal adenocarcinoma	PK-8 cells		CVCL_4718
Experiment 3 Reporting the Activity Date of This ADC					[195]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[196]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 24)	Positive CDCP1 expression (CDCP1 +++/++)
Method Description	Mice were randomized into groups of six and administered a single intravenous treatment of 10D7 MMAE (5 mg/kg), 10D7 (5 mg/kg), MMAE (0.17 mg/kg; equivalent to a four molar excess of the 10D7-MMAE dose) or vehicle.
In Vivo Model	Ovarian cancer PDX model (PDX: PH250)

Experiment 1 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 56)	High PODXL expression (PODXL+++)
Method Description	MIA PaCa-2 (1x106) or OV3331 (1x106) cells were injected subcutaneously into the right flank of NSG or nude mice. Tumor dimensions were measured twice a week and tumor volumes (cm3) were calculated by. Once tumors reached 0.15cm3, mice were treated with either PODO447- or palivizumab-Vedotin at concentrations ranging from 4 2 mg/kg. ADC treatments were administered intravenously every 4 days.    Click to Show/Hide
In Vivo Model	Pancreas cancer PDX model (PDX: MIA PaCa-2)

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 40)	Negative EGFR expression (EGFR -)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	NCI-H2228 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.65% (Day 40)	Positive EGFR expression (EGFR +++/++)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM±0.10 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 40)	Negative EGFR expression (EGFR -)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	NCI-H2228 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.65% (Day 40)	Positive EGFR expression (EGFR +++/++)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM±0.10 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

Experiment 1 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 27)	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with c1F6-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of c1F6-9a at 3 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.45 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30.00 nM	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 3 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 35)	Moderate EGFR expression (EGFR ++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 0.3 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	LoVo CDX model
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.00% (Day 18)	Positive EGFR expression (EGFR +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.00% (Day 18)	Positive EGFR expression (EGFR +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 5 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.70% (Day 35)	Moderate EGFR expression (EGFR ++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	LoVo CDX model
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.60% (Day 35)	Moderate EGFR expression (EGFR ++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	LoVo CDX model
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.10 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Colorectal carcinoma	DiFi cells		CVCL_6895
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.80 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Colorectal carcinoma	DiFi cells		CVCL_6895
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	611.00 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.20 ug/mL	Moderate EGFR expression (EGFR ++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.30 ug/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 6 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28.30 ug/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 18.98% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.28% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.70% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.30% (Day 43)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.51% (Day 43)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.57% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.92% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.81% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.92% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 11 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.77% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 12 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.10% (Day 77)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted MDAMB-468 breast cancer tumor cells, and show responsiveness against the MDA-MB-468 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 13 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.25% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.74 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.89 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.38 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.80 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.59 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0.00% (Day 28)	Moderate LRRC15 expression (LRRC15++; IHC 2+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in MC-38 xenografts.
In Vivo Model	MC-38 CDX model
In Vitro Model	Mouse colon adenocarcinoma	MC-38 cells		CVCL_B288
Experiment 2 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	59.41% (Day 38)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in HPAF-II xenografts.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 3 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	64.94% (Day 23)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 4 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	71.99% (Day 11)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 5 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	80.57% (Day 28)	Moderate LRRC15 expression (LRRC15++; IHC 2+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus anti-PD1 mAb (2 mg/kg) were demonstrated in MC-38 xenografts.
In Vivo Model	MC-38 CDX model
In Vitro Model	Mouse colon adenocarcinoma	MC-38 cells		CVCL_B288
Experiment 6 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	87.45% (Day 78)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in NW-231 xenografts.
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 7 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.36 % (Day 26)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (4.5 mg/kg) was demonstrated in HN-5 xenografts.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 8 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.55% (Day 23)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus Carboplatin (50 mg/kg) were demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 9 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	89.39% (Day 72)	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in PANC-1 xenografts.
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 10 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	89.73% (Day 23)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus Cetuximab (3 mg/kg) were demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 11 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90.12% (Day 30)	Moderate LRRC15 expression (LRRC15++; IHC 2+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in NW-231 xenografts.
In Vivo Model	NW-231 CDX model
In Vitro Model	Triple negative breast cancer	NW231 cells		Homo sapiens
Experiment 12 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.24% (Day 21)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 13 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.66% (Day 18)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 14 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.84% (Day 27)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in SCC-15 xenografts.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 15 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.86% (Day 21)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 16 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.25% (Day 23)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus Radiation (15 Gy) were demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 17 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.71% (Day27)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in NCI-H1650 xenografts.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 18 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	93.56% (Day 38)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) plus Gemcitabine (80 mg/kg) were demonstrated in HPAF-II xenografts.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 19 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.35% (Day 33)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in NCI-H1650 xenografts.
In Vivo Model	HN-5 CDX model
In Vitro Model	Squamous cell carcinoma	HN-5 cells		CVCL_8128
Experiment 20 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	97.05 % (Day 16)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 21 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.10% (Day 21)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) plus Gemcitabine (100 mg/kg) were demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 22 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.18% (Day 27)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) plus Erlotinib (100 mg/kg) were demonstrated in SCC-15 xenografts.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 23 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.13% (Day 18)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (3 mg/kg) plus Docetaxel (7.5 mg/kg) were demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 3.53% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.69% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.02% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.11% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.13% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.51% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.40 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.27% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.47% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.64% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.70% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.36% (Day 43)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.15% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.31% (Day 43)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.67% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.74% (Day 77)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted MDAMB-468 breast cancer tumor cells, and show responsiveness against the MDA-MB-468 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.27% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 11 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.12% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 12 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.55% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 13 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.28% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.00 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	59.00 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90.00 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.56 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.77 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.54% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	128.50 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	11.00% (Day 26)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-vcMMAE-DAR4 (10 mg/kg) was demonstrated in HCC-827-ER xenografts.
In Vivo Model	HCC-827-ER CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 ER1 cells		CVCL_EJ07
Experiment 2 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	59.49% (Day 60)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-vcMMAE-DAR4 (3 mg/kg) was demonstrated in SUM190PT xenografts.
In Vivo Model	SUM190PT CDX model
In Vitro Model	Breast inflammatory carcinoma	SUM190PT cells		CVCL_3423
Experiment 3 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	84.03% (Day 21)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-vcMMAE-DAR4 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 11.64% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 0.25 mg/kg of ADC9.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.60% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg of ADC9.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.50 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.58 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 3 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.05 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.26 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 5 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.81 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 12.50% (Day 10	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 2 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.63% (Day 20)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.63% (Day 20)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.17% (Day 10)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 5 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50% (Day 20)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 6 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 10)	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 7 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Median survival time (MST)	14 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 8 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Median survival time (MST)	23 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 9 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Median survival time (MST)	24 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 10 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Median survival time (MST)	30 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 11 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Median survival time (MST)	60 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 12 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Median survival time (MST)	61 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480

Experiment 1 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.00 pM	Positive EGFR expression (EGFR +++/++)
Method Description	MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.38 nM	Positive EGFR expression (EGFR +++/++)
Method Description	MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.21% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 14.62% (Day 43)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 25.99% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.46% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.91% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.04% (Day 43)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.42% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.12% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.78% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.78% (Day 91)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 11 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.90% (Day 77)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted MDAMB-468 breast cancer tumor cells, and show responsiveness against the MDA-MB-468 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 12 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.77% (Day 49)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 13 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.44% (Day 70)	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.00 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30.00 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	43.00 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 24.70% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.50% (Day 51)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.90% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg QDx1 of ADC2.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.36% (Day 35)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm3 on average (Day 1), and 3 mg/kg QWx4 of ADC2.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.43% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 4 mg/kg of ADC2.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 4 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.22% (Day 33)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing mantle cell lymphoma cell line JeKo-1 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm3 on average (Day 1), and 3 mg/kg QWx4 of ADC2.
In Vivo Model	JeKo-1 CDX model
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 5 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.81% (Day 41)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing breast cancer cell line HCC1187 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm3 on average (Day 1), and 0.31 mg/kg QWx4 of ADC5.
In Vivo Model	HCC1187 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.59 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.57 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.53 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 4 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.91 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 5 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.28 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.70% (Day 13)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 0.7 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.30% (Day 13)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 2 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 58)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3.75 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.00% (Day 13)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 7 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.60% (Day 20)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3.75 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 58)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 15 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 7 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 20)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 15 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.49 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 6 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 7 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 8 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 9 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.10% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 2 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.10% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 2 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.20% (Day 30)	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-1c25E, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder carcinoma	RT-4 cells		CVCL_0036

Experiment 1 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.50% (Day 21)	High MUC1 expression (MUC1+++)
Method Description	To examine the efficacy of the HzMUC1-MMAE in decreasing pancreatic tumor growth in vivo,pancreatic tumor xenograft mouse model was established. BALB/c nu/nu mice were subcutaneously injected with CFPAC-1 cells. When the CFPAC-1 tumors reached the sizes of 150 mm3,mice were randomized into two groups and treated with PBS and HzMUC1-MMAE (5 mg/kg,every 6 days,for 2 doses).    Click to Show/Hide
In Vivo Model	Pancreatic cancer CDX model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.10% (Day 28)	High MUC1 expression (MUC1+++)
Method Description	To examine the efficacy of the HzMUC1-MMAE in decreasing pancreatic tumor growth in vivo,pancreatic tumor xenograft mouse model was established. BALB/c nu/nu mice were subcutaneously injected with Capan-2 cells. When the Capan-2 tumors reached the sizes of 120 mm3,mice were randomized into two groups and treated with PBS and HzMUC1-MMAE (5 mg/kg,every 6 days,for 2 doses).    Click to Show/Hide
In Vivo Model	Pancreatic cancer CDX model
In Vitro Model	Pancreatic cancer	Pancreatic cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 nM	High MUC1 expression (MUC1+++)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-2 cells		CVCL_0026
Experiment 2 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50.00 nM	High MUC1 expression (MUC1+++)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	CFPAC-1 cells		CVCL_1119
Experiment 3 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	59.00 nM	Moderate MUC1 expression (MUC1++)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 uM	Negative MUC1 expression (MUC1-)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic adenocarcinoma	SW1990 cells		CVCL_1723

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.39% (Day 28)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.15% (Day 57)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.21% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.21% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.94% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.80 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	41.21% (Day 30)	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	1 mg conjugate/kg/inj.
In Vivo Model	Karpas 299 ALCL cell line xenograft model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.67% (Day 40)	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	3 mg conjugate/kg/inj.
In Vivo Model	L2987 cell line xenograft model
In Vitro Model	Lung adenocarcinoma	L2987 cells		CVCL_H586
Experiment 3 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.60% (Day 40)	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	3 mg conjugate/kg/inj.
In Vivo Model	L2987 cell line xenograft model
In Vitro Model	Lung adenocarcinoma	L2987 cells		CVCL_H586

Experiment 1 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =2,111)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =3,500)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =755)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Breast carcinoma	H3396 cells		CVCL_D348
Experiment 4 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.00 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =922)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Amelanotic melanoma	MDA-MB-435 cells		CVCL_0417
Experiment 5 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.00 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =600)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Colon carcinoma	RCA cells		CVCL_R735
Experiment 6 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.00 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =645)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.77% (Day 28)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.85% (Day 57)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.00% (Day 14)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80% (Day 36)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 36)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 14)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 36)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC38 cells		CVCL_1267
Experiment 6 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 7 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 8 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.70% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	234 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	49.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	93.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	27.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (43D7-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 49.63% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 0.25 mg/kg of 2A2 dPBD ADC.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg of 2A2 dPBD ADC.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1000 pM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.48 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.43 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.60% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.85% (Day 18)	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.60% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.85% (Day 18)	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.93% (Day 26)	Positive CLDN1 expression (CLDN1 +++/++)
Method Description	100,000 SW620 cells were suspended in culture medium and Matrigel (v/v) and injected subcutaneously into the right flank of 6-week-old female athymic nude mice. When the tumor volume reached approximately 100 mm3, mice were randomized in different groups. For ADC experiments, mice received by iv injection 0.9% NaCl or ADCs (5 mg/kg per injection) twice per week for 4 weeks.    Click to Show/Hide
In Vivo Model	SW620 CDX model
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.59% (Day 22)	Positive CLDN1 expression (CLDN1 +++/++)
Method Description	100,000 SW620 cells were suspended in culture medium and Matrigel (v/v) and injected subcutaneously into the right flank of 6-week-old female athymic nude mice. For the sequential combination experiments, mice received oxaliplatin at 3 mg/kg once per week followed by an iv injection of ADC-6F6 at 5 mg/kg after 3 and 6 days.
In Vivo Model	SW620 CDX model
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.00% (Day 14)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.70% (Day 40)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 0.3 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 14)	Positive TF expression (TF +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.80% (Day 40)	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 5 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC38 cells		CVCL_1267
Experiment 7 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 8 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 9 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480

Experiment 1 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.40% (Day 16)	Positive LRG1 expression (LRG1+++/++)
Method Description	Single-cell suspensions of 1 x106 B16F0 cells were injected subcutaneously into the lower back of Lrg1+/+ C57BL/6 mice in 100 mL PBS. Tumours were measured and therapy was initiated when tumour volumes reached 0.1 cm3. ADC was administered at a dose of 20 mg/kg treatments were administered by a single intraperitoneal injection every 7 days for 3 weeks.    Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Melanoma	Melanoma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.90 nM	Positive LRG1 expression (LRG1+++/++)
Method Description	5 x104 cells were seeded in 96-well plates and incubated at 37 overnight. Cells were thenexposed to a range of concentrations of the test compounds diluted in growth medium at pH 6.5 and at 37 as ADC 5 (0100 nM, 72 h). MTT reagent (12 mM) was then added to each well and cells were incubated for 4 h at 37 , followed by the addition of DMSO and further incubation at 37 1C for 1 h.    Click to Show/Hide
In Vitro Model	Mouse melanoma	B16-F0 cells		CVCL_0604

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.70% (Day 21)	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	46.70 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.99% (Day 36)	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.50% (Day 36)	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.00% (Day 30)	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-1abe16E, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.18% (Day 28)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50% (Day 57)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.90% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.60% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.49% (Day 21)	Negative HER2 expression (HER2-)
Method Description	The nude mice were implanted with a human cancer cell line(MDA-MB-231) and the ADCs (10 mg/kg) were administered through intraperitoneal injection when the tumor volume reached about 100 cubic millimeters. The tumor volumes were monitored every 3 days and animals were sacrificed at the end of 21 days and the tumors were dissected and weighed.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.80% (Day 21)	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.36% (Day 21)	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.05% (Day 5)	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 3 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 4 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.92% (Day 21)	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.87 nM	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.26 nM	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	786.00 nM	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric carcinoma	HGC-27 cells		CVCL_1279

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.61% (Day 28)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.75% (Day 51)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.70% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.76% (Day 25)	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (1 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70% (Day 25)	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.50% (Day 25)	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (10 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 4 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.50% (Day 25)	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623

Experiment 1 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.10 pM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Breast carcinoma	MDA-MB-157 cells		CVCL_0618
Experiment 3 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	63.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	69.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	18.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (25G1-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.68% (Day 43)	Positive GD2 expression (GD2+++/++)
Method Description	When tumors reached 50 mm3 volume. Three groups received intravenous injections of 100 ug (5 mg/kg) ch14.18-MMAE, ch14.18-MMAF, or naked antibody for five times with an interval of 4 days, and the control group was injected with PBS.
In Vivo Model	B78-D14 CDX model
In Vitro Model	Amelanotic melanoma	B78-D14 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Thymoma	EL4 cells		CVCL_0255
Experiment 2 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	IMR-32 cells		CVCL_0346
Experiment 3 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	COLO 38 cells		CVCL_3934
Experiment 4 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	B78-D14 cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.51 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Pleural malignant mesothelioma	MS-1 [Human mesothelioma] cells		CVCL_E993
Experiment 6 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556
Experiment 7 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 8 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.93 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	Hs 578T cells		CVCL_0332
Experiment 9 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.48 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Bone marrow neuroblastoma	SH-SY5Y cells		CVCL_0019
Experiment 10 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.28 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Astrocytoma	1321N1 cells		CVCL_0110
Experiment 11 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.80 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 12 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.40 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 13 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.10 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	MG-63 cells		CVCL_0426
Experiment 14 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	NGP-127 cells		CVCL_UF75
Experiment 15 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40.00 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 16 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	HOS cells		CVCL_0312
Experiment 17 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 18 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Melanoma	B16 cells		CVCL_F936
Experiment 19 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	M3 cells		CVCL_4Y25
Experiment 20 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.09 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Thymoma	EL4 cells		CVCL_0255
Experiment 21 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.14 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	COLO 38 cells		CVCL_3934
Experiment 22 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.15 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	IMR-32 cells		CVCL_0346
Experiment 23 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.20 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Pleural malignant mesothelioma	MS-1 [Human mesothelioma] cells		CVCL_E993
Experiment 24 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.22 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	B78-D14 cells		Homo sapiens
Experiment 25 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.23 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556
Experiment 26 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.28 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 27 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.38 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	Hs 578T cells		CVCL_0332
Experiment 28 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.48 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Astrocytoma	1321N1 cells		CVCL_0110
Experiment 29 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.51 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Bone marrow neuroblastoma	SH-SY5Y cells		CVCL_0019
Experiment 30 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	2.70 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 31 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	2.98 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	MG-63 cells		CVCL_0426
Experiment 32 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	3.00 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 33 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	8.47 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 34 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	17.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Melanoma	B16 cells		CVCL_F936
Experiment 35 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	NGP-127 cells		CVCL_UF75
Experiment 36 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	HOS cells		CVCL_0312
Experiment 37 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 38 Reporting the Activity Date of This ADC					[215]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20.00 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	M3 cells		CVCL_4Y25

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.30% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.72% (Day 52)	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.72% (Day 52)	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.63% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.63% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	68.00% (Day 49)	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	24.00 nM	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (25A3-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.34% (Day 60)	High HER2 expression (HER2 +++)
Method Description	An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (5 mg/kg) on days 0, 7, 14, and 21.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.21% (Day 60)	High HER2 expression (HER2 +++)
Method Description	An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (10 mg/kg) on days 0, 7, 14, and 21.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2 +++)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2 +++)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2 +++)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	97.62 nM	Negative HER2 expression (HER2-)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	110.54 nM	Negative HER2 expression (HER2-)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	70.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	42.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (43B1-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.42% (Day 56)	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50.00 nM-500.00 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.92% (Day 56)	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50.00 nM-500.00 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.19% (Day 24)	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg HLvM4 was intravenously administered once every three days for three weeks.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.33% (Day 24)	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg HLvM4 was intravenously administered once every three days for three weeks.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	40.53 nM	Positive DLL4 expression (DLL4 +++/++)
Method Description	In vitro cytotoxicity and mechanism of anti-DLL4 ADCs. The cytotoxicity of ADCs was assessed by MTT assay. The percentage of cell inhibition relative to untreated control HUVEC cells was calculated for each drug concentration.
In Vitro Model	Normal	HUVEC-C cells		CVCL_2959

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.65% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.65% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75.00% (Day 73)	Low HER2 expression (HER2+)
Method Description	1A3-MMAE=5 mg/kg.
In Vivo Model	MCF7 breast cancer xenograft model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 21)	Low HER2 expression (HER2+)
Method Description	1A3-MMAE=5 mg/kg.
In Vivo Model	MCF7-F breast cancer xenograft model
In Vitro Model	Invasive breast carcinoma	MCF7-F (fulvestrant resistant) cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.82% (Day 28)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.97% (Day 57)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.90% (Day 37)	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (2.5 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H69 CDX model
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.50% (Day 37)	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (5 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H69 CDX model
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 37)	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 4 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.00% (Day 37)	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 5 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 37)	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H69 CDX model
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 6 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 37)	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive CD56 expression (CD56 +++/++)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.23 nM	Positive CD56 expression (CD56 +++/++)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.24 nM	Positive CD56 expression (CD56 +++/++)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H524 cells		CVCL_1568
Experiment 4 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1200 nM	Negative CD56 expression (CD56 -)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Normal	NK cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.49% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.49% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.00% (Day 60)	High HER2 expression (HER2+++)
Method Description	Mil40-12b induces efficient tumor cell killing in cell PDX models from a breast cancer patient with HER2 expression.
In Vivo Model	Breast ductal carcinoma CDX model
In Vitro Model	Breast ductal carcinoma	Breast ductal carcinoma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.80 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	53.60 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	102.60 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	207.40 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.52 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.44 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[221]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.00% (Day 27)	High PIEZO1 expression (PIEZO1+++)
Method Description	1 x107 TE1 cells were suspended in Matrigel and injected subcutaneously in the right armpit. The treatment of AntiPIEZO1MMAE or control reagents started when the tumor volume reached 300mm3. Treatments for each group were given every 3 days in total four times.
In Vivo Model	Esophageal squamous cell carcinoma CDX model
In Vitro Model	Esophageal squamous cell carcinoma	Esophageal squamous cell carcinoma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.21% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.21% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.63% (Day 56)	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.85% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.85% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.83% (Day 67)	Positive HER2 expression (HER2+++/++)
Method Description	Nude mice were implanted with SK-OV-3 tumor cells which were allowed to establish tumors of ~150 mm3 prior to initiation of treatment. ADCs at 10 mg/kg doses were injected through tail vein on days 38, 45, 52 and 59. There were ~10 mice per group. The tumor volume of mice in different group was measured and their survival was recorded.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.70 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.10% (Day 30)	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-10ac14E, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.40% (Day 25)	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10% (Day 29)	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	Detroit 562 CDX model
In Vitro Model	Pharyngeal squamous cell carcinoma	Detroit 562 cells		CVCL_1171

Experiment 1 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	86.91% (Day 21)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huAD208.4.1-vcMMAE-DAR4 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.40% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 2 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.40% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 2 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[224]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50% (Day 30)	Positive PSMA expression (PSMA +++/++)
Method Description	In order to specify the pharmacological properties of MMAE.VC.SA.617 we inoculated LNCaP cells into NOD/SCID mice to generate a xenograft model. In vivo therapeutic efficacy studies were conducted with MMAE.VC.SA.617, namely 1.0 mg/kg (corresponding to 0.49 mg MMAE).
In Vivo Model	LNCaP CDX model
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80% (Day 18)	High GSDME expression (GSDME +++)
Method Description	Comparison of the maximum tested dose of mesoADC (4.4 mg/kg) to PBS vehicle or isotype control ADC confirmed the antitumor effectiveness of the ADC up to day 18 .
In Vivo Model	EMT6 CDX model
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 ug/mL	High GSDME expression (GSDME +++)
Method Description	EMT6 cells were pulsed with 1 ug/mL mesoADC for 30min then chased for 30 and 60min at 37°C.
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923
Experiment 2 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.50 ug/mL	Low GSDME expression (GSDME +)
Method Description	CT26 cells were pulsed with 1 ug/mL mesoADC for 30min then chased for 30 and 60min at 37°C.
In Vitro Model	Colon carcinoma	CT26 cells		CVCL_7254

Experiment 1 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.93% (Day 29)	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	Detroit 562 CDX model
In Vitro Model	Pharyngeal squamous cell carcinoma	Detroit 562 cells		CVCL_1171
Experiment 2 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.94% (Day 25)	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.73% (Day 45)	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 250 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for 3 mg/kg very four days for a total of 5 doses.
In Vivo Model	M28 CDX model
In Vitro Model	Pleural malignant mesothelioma	M28K cells		CVCL_8106
Experiment 2 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.89% (Day 45)	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 250 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for 5 mg/kg very four days for a total of 5 doses.
In Vivo Model	M28 CDX model
In Vitro Model	Pleural malignant mesothelioma	M28K cells		CVCL_8106

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.30 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Pleural malignant mesothelioma	M28K cells		CVCL_8106
Experiment 2 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.44 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Pleural sarcomatoid mesothelioma	VAMT-1 cells		CVCL_A731
Experiment 3 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Normal	HK-2 [Human kidney] cells		CVCL_0302
Experiment 4 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Normal	HS775Li cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Normal	HS-27 cells		CVCL_0E34

Experiment 1 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90.12% (Day 21)	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huAD208.14.1-vcMMAE-DAR4 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.20% (Day 32)	Positive MRC2 expression (MRC2 +++/++)
Method Description	Vehicle (PBS) or 10 mg/kg of A5/158-vc-MMAE were administered into the lateral tail vein of mice twice a week for 2 weeks. Primary tumors were weighed at necropsy.
In Vivo Model	MG-63-mChLuc2 CDX model
In Vitro Model	Osteosarcoma	MG-63 cells		CVCL_0426

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00% (Day 39)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (39A-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.91% (Day 56)	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.97% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.97% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.60% (Day 32)	High HER2 expression (HER2+++)
Method Description	The animals were given vehicle, mil40, and ADC on days 0, 7, 14, and 21, and 4 intravenous injections of ADC at doses of 5 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Maximum inhibition efficiency (MIE)	< 10.00%	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Maximum inhibition efficiency (MIE)	47.80%	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Maximum inhibition efficiency (MIE)	50.50%	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.30%	Moderate HER2 expression (HER2++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 5 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Maximum inhibition efficiency (MIE)	93.54%	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Moderate HER2 expression (HER2++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 8 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.74 nM	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.34% (Day 28)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.45% (Day 51)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.00% (Day 21)	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 10)	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 17)	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (1.5 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 17)	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (0.75 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High MSLN expression (MSLN+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal Effective Concentration (EC50)	153.50 ng/mL	High MSLN expression (MSLN+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.28% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.28% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.28% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.28% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.79% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.79% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.77% (Day 18)	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.77% (Day 18)	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10% (Day 35)	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70% (Day 35)	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Non-small cell lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70% (Day 35)	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 4 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.50% (Day 32)	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Astrocytic glioblastoma CDX model
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.27% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.27% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Tumor Growth Inhibition value (TGI)	97.00% (Day 49)	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Low FOLR1 expression (FOLR1+)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (29E-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.02% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.02% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.23% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.23% (Day 29)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.64% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.64% (Day 25)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.76% (Day 67)	Positive HER2 expression (HER2+++/++)
Method Description	Nude mice were implanted with SK-OV-3 tumor cells which were allowed to establish tumors of ~150 mm3 prior to initiation of treatment. ADCs at 10 mg/kg doses were injected through tail vein on days 38, 45, 52 and 59. There were ~10 mice per group. The tumor volume of mice in different group was measured and their survival was recorded.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.30 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.90% (Day 18)	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.95% (Day 57)	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 21)	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High MSLN expression (MSLN+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 42)	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 27)	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with cAC10-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of cAC10-9a at 0.75 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 27)	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with cAC10-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of cAC10-9a at 1 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 3 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 27)	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with cAC10-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of cAC10-9a at 3 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 55.00 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 40)	Positive RON expression (RON +++/++)
Method Description	Treatment began when tumors reached a mean tumor volume of 100 to 150 mm3. Zt/g4-MMAE or Zt/g4-DM1 at 20 mg/kg in a Q12 2 regimen was injected through the tail vein.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 50)	Positive MUC16 expression (MUC16 +++/++)
Method Description	In vivo efficacy of MUC16 targeting ADCs in the Ovcar3 tumor model. 3A5-mc-VC-PAB-MMAE ADC dosed at 5 mg/kg (in each study with the exact dosing for control) IV in SCID mice.
In Vivo Model	OVCR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.82 nM	Positive MUC16 expression (MUC16 +++/++)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative MUC16 expression (MUC16-)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Normal	HEK293 cells		CVCL_0045

Experiment 1 Reporting the Activity Date of This ADC					[233]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 52)	High EGFR expression (EGFR+++)
Method Description	For the tumor xenograft model, 5.0x106 MDA-MB-468 cells or 3.0x106 MDA-MB-231 cells were injected subcutaneously into the right flank of each 6 week-old female BALB/c nude mice. when the tumor volumes reached approximately 100 mm3 (approximately 8 days), the 24 mice were randomly divided into 4 groups (6 mice per group): control group, LR004 antibody group, LR004-VC-MMAE group, and doxorubicin (positive control) group, which were treated with PBS or different drugs (LR004 antibody 10 mg/kg, LR004-VC-MMAE 10 mg/kg, doxorubicin 2 mg/kg) every 5 days for 4 times through i.v. injections.    Click to Show/Hide
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 49)	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 33)	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	53.68% (Day 36)	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	89.84% (Day 36)	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	64.86% (Day 52)	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	95.44% (Day 52)	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.00 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Low FOLR1 expression (FOLR1+)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (54E-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Low FOLR1 expression (FOLR1+)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.00 nM	Low FOLR1 expression (FOLR1+)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[236]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.98 ng/mL±0.74 ng/mL	Positive HER3 expression (HER3+++/++)
Method Description	Cells were plated in 96-well flat-bottom plates the day before starvation in 1% FCS for 24hr. HER3-ADC at different dilutions was then added for 5 days, with 50ng/ml NRG1. In the absence of NRG1 stimulation, cells were maintained in 10% FCS and treated with HER3-ADC.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.10% (Day 18)	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 2 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.29 ug/mL±0.28 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 3 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.20 ug/mL±2.01 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	MAVER-1 cells		CVCL_1831
Experiment 4 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.69 ug/mL±0.29 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	Z-138 cells		CVCL_B077
Experiment 5 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.78 ug/mL±2.15 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	8.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	65.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	72.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	80.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	84.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	162 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.32 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	32.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	72.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	78.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	79.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	80.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	86.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	33.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	72.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	86.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	88.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	104 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.10 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.64 uM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	36.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	74.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	76.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	90.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	64.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	369 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	678 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	41.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	71.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	77.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	78.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	81.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	46.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	75.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	76.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	78.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	80.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	81.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.37 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	48.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	77.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	84.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	88.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	56.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	215 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.62 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	50.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	70.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	75.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	80.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	80.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.41 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	69.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	73.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	95.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	856 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	74.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	81.00%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 3 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	84.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 4 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	89.00%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Maximum inhibition efficiency (MIE)	93.00%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 7 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 8 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 10 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52.00 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.14 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	89.00%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	96.00%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.63 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70.00 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	90.00%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	96.00%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.60 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70.00 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	90.00%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	96.00%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.28 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70.00 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	91.00%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Max inhibition rate (MIR)	97.00%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.39 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.28 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70.00 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Inhibition rate (50 nM)	90.00%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.70 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 20.00 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[240]
Efficacy Data	80% Effective Dose (ED80)	3.60 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Inhibition rate (50 nM)	91.00%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.00 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.90 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[240]
Efficacy Data	80% Effective Dose (ED80)	4.40 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Inhibition rate (50 nM)	92.00%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.10 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.00 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[240]
Efficacy Data	80% Effective Dose (ED80)	0.70 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Inhibition rate (50 nM)	93.00%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.40 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 19.00 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[240]
Efficacy Data	80% Effective Dose (ED80)	2.10 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.70 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.90 pM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	98.00 pM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	INA-6 cells		CVCL_5209
Experiment 3 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.60 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	KMS-12-BM cells		CVCL_1334
Experiment 5 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30.10 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Multiple myeloma	SK-MM-1 cells		CVCL_A478
Experiment 6 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	46.10 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	OCI-My5 cells		CVCL_E332
Experiment 7 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60.90 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	OCI-My7 cells		CVCL_E333
Experiment 8 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	JIM3 cells		CVCL_2533
Experiment 9 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	LP-1 cells		CVCL_0012
Experiment 10 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 uM	Positive SEMA4A expression (SEMA4A +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Plasma cell myeloma	OPM-2 cells		CVCL_1625

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.10 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.20 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34.00 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.40 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	41.60 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	53.90 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	59.90 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	88.00 pM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.90 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 5 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM±0.001 nM	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 6 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 7 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM±0.04 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.71 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.07 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.31 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.14 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.71 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.07 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.31 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.14 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.51 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.44 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 2 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 2 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM±0.01 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.62 nM±0.08 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive CD19 expression (CD19+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive CD19 expression (CD19+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive CD19 expression (CD19+++/++)
Method Description	Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative CD19 expression (CD19-)
Method Description	K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM±0.01 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM±0.02 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM±0.21 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM±0.01 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM±0.02 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78 nM±0.02 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive CD19 expression (CD19+++/++)
Method Description	Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative CD19 expression (CD19-)
Method Description	Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM
Method Description	Cytotoxicity of non-irradiated or X-ray-irradiated (8 Gy) mAb-DMBA-SIL-MMAE conjugate in comparison to free MMAE in anaplastic thyroid cancer.
In Vitro Model	Thyroid gland anaplastic carcinoma	8505C cells		CVCL_1054

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.80 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.01 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.40 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Moderate EGFR expression (EGFR++)
Method Description	The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Low EGFR expression (EGFR+)
Method Description	The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.52 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Moderate EGFR expression (EGFR++)
Method Description	The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative EGFR expression (EGFR-)
Method Description	The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.63 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.87 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19±0.05 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	High FOLR1 expression(FOLR1+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530
Experiment 3 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low FOLR1 expression(FOLR1+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative FOLR1 expression(FOLR1-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	SJSA-1 cells		CVCL_1697

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	High ITGA2B expression (ITGA2B+++/++)
Method Description	The MTT-based cytotoxicity assay in MDA-MB-231 cells that displayed a dose dependent cell killing of ADC treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.51 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.63 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	45.00 nM	Moderate HER2 expression (HER2++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.20 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22±0.01 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 8 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	241 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.63 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.00 nM	Moderate HER2 expression (HER2++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	241.00 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275.00 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.61 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.52 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 5 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.10 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.33 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 7 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.10 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.15 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 9 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.98 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 10 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Thyroid gland anaplastic carcinoma	8505C cells		CVCL_1054
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Mouse colon adenocarcinoma	MC-38 cells		CVCL_B288
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.29 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Acute erythroid leukemia	TBP-3743 cancer cells		Mus musculus
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.92 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Oral cavity squamous cell carcinoma	MOC-L2 cells		CVCL_A9X4
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 nM±0.10 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

Experiment 1 Reporting the Activity Date of This ADC					[256]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.89 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	SNU-16, NCI-H716 and U2OS cells were seeded at a density of 5000 cells per well in a 96-well culture plate and treated with vcMMAE, scFvF7-Fc, or antibody-vcMMAE conjugate scFvF7-Fc-MMAE for 96 hours.
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[256]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.70 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	SNU-16, NCI-H716 and U2OS cells were seeded at a density of 5000 cells per well in a 96-well culture plate and treated with vcMMAE, scFvF7-Fc, or antibody-vcMMAE conjugate scFvF7-Fc-MMAE for 96 hours.
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581

Experiment 1 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[257]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-2.00 nM	Positive KAAG1 expression (KAAG1 +++/++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four multiple human cancer cell lines.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[257]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-2.00 nM	Positive KAAG1 expression (KAAG1 +++/++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four multiple human cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[257]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-2.00 nM	Positive KAAG1 expression (KAAG1 +++/++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four multiple human cancer cell lines.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035

Experiment 1 Reporting the Activity Date of This ADC					[258]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-10.00 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoma	HEK293T cells (ENPP1 expression)		CVCL_0063
Experiment 2 Reporting the Activity Date of This ADC					[258]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative ENPP1 expression (ENPP1-)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Normal	HEK293T cells		CVCL_0063
Experiment 3 Reporting the Activity Date of This ADC					[258]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027

Experiment 1 Reporting the Activity Date of This ADC					[258]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM-10.00 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoma	HEK293T cells (ENPP1 expression)		CVCL_0063
Experiment 2 Reporting the Activity Date of This ADC					[258]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	65.00 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[258]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative ENPP1 expression (ENPP1-)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Normal	HEK293T cells		CVCL_0063

Experiment 1 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.45 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.47 nM	Positive CD20 expression (CD20+++/++)
Method Description	Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 nM	Positive CD20 expression (CD20+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.13 nM	Positive CD20 expression (CD20+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative CD20 expression (CD20-)
Method Description	K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.47 nM	Positive CD20 expression (CD20+++/++)
Method Description	Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.30 nM	Negative CD20 expression (CD20-)
Method Description	Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.40 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[259]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.45 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[259]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.13 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[259]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.58 nM	Moderate EGFR expression (EGFR++)
Method Description	1 x104 cells per well in a volume of 100 ull were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 4 Reporting the Activity Date of This ADC					[259]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.80 nM±1.40 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 3 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[260]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.20 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[260]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.30 nM±2.70 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 3 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 nM±5.90 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	487.00 nM±194.00 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 4 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[261]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 nM	Positive CD4 expression (CD4 +++/++)
Method Description	Receptors (R2) as a function of ADC concentrations, upon incubation with the antibody and following additional 48 h.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 2 Reporting the Activity Date of This ADC					[261]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 nM	Positive CD4 expression (CD4 +++/++)
Method Description	Receptors (R1) as a function of ADC concentrations, upon incubation with the antibody and following additional 48 h.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 3 Reporting the Activity Date of This ADC					[261]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	40.00 nM	Positive CD4 expression (CD4 +++/++)
Method Description	Receptors (R4) as a function of ADC concentrations, upon incubation with the antibody and following additional 48 h.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34.00 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50.00 nM	Positive MSL expression (MSL+++/++)
Method Description	The cells were incubated in a CO2 incubat or with saturated water overnight, On the second day, two covalent thiol conjugated ADCs were serially diluted conjugates were added to the 96 well plate containing OVCAR3 cells, 100uL per well. The initial conjugate was 100000 ng/ml and diluted to 0.001 ng/ml. OVCAR3 cells with added ADC were incubated at 37 for 72 hours.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66.00 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 300.00 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	382.40 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	682.40 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	265.30 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 2 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 663.08 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 3 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 663.08 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 663.08 nM	Negative PD-L1 expression (PD-L1-)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPC-1 cells		CVCL_0152

Experiment 1 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	272.10 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 2 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 653.93 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 3 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 653.93 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 653.93 nM	Negative PD-L1 expression (PD-L1-)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPC-1 cells		CVCL_0152

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 ng/mL	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD30 expression (CD30+++/++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	65.00 ng/mL	Moderate CD30 expression (CD30++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361
Experiment 4 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Negative CD30 expression (CD30-); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.70 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.80 ng/mL	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD30 expression (CD30+++/++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 4 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.94 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	57.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	57.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.23 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[264]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.70 ng/mL	High HER2 expression (HER2+++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[264]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.10 ng/mL	High HER2 expression (HER2+++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[264]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.10 ng/mL	High HER2 expression (HER2+++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.00 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 3 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD30 expression (CD30+++/++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[263]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.00 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[265]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 ug/mL	Positive VEGFA expression (VEGFA +++/++)
Method Description	The anti-proliferative activity of Bevacizumab Vedotin and Bevacizumab against three different cell lines was determined by MTT method.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[265]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 ug/mL	Positive VEGFA expression (VEGFA +++/++)
Method Description	The anti-proliferative activity of Bevacizumab Vedotin and Bevacizumab against three different cell lines was determined by MTT method.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[265]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.17 ug/mL	Positive VEGFA expression (VEGFA +++/++)
Method Description	The anti-proliferative activity of Bevacizumab Vedotin and Bevacizumab against three different cell lines was determined by MTT method.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[266]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.55 nM	High FGFR1 expression (FGFR1+++)
Method Description	Human lung cancer cell lines showing FGFR1 overexpression (NCI-H520 and NCI-H1581) was chosen and a cell line with physiological, low levels of FGFR1 (HCC95) was chosen as a control,.
In Vitro Model	Lung large cell carcinoma	NCI-H1581 cells		CVCL_1479
Experiment 2 Reporting the Activity Date of This ADC					[266]
Efficacy Data	Half Maximal Effective Concentration (EC50)	90.49 nM	High FGFR1 expression (FGFR1+++)
Method Description	Human lung cancer cell lines showing FGFR1 overexpression (NCI-H520 and NCI-H1581) was chosen and a cell line with physiological, low levels of FGFR1 (HCC95) was chosen as a control,.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 3 Reporting the Activity Date of This ADC					[266]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000.00 nM	Negative FGFR1 expression (FGFR1-)
Method Description	Human lung cancer cell lines showing FGFR1 overexpression (NCI-H520 and NCI-H1581) was chosen and a cell line with physiological, low levels of FGFR1 (HCC95) was chosen as a control,.
In Vitro Model	Lung squamous cell carcinoma	HCC95 cells		CVCL_5137

Experiment 1 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.75 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 2 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Effective Concentration (EC50)	10.33 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[262]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.94 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	71.60 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Colorectal carcinoma	DiFi cells		CVCL_6895

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Effective Concentration (EC50)	72.60 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Colorectal carcinoma	DiFi cells		CVCL_6895

Experiment 1 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 nM 7.13 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 nM 8.79 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 nM 12.68 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[267]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.10 nM 16.05 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 nM 10.67 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.41 nM 6.20 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 nM 6.08 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 nM 11.07 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 nM 6.39 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 nM 10.67 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 nM 7.06 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[268]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 nM 11.07 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[269]
Efficacy Data	Partial Response (PR)	7.84% (patients with NSCLC, active doses 1.8 mg/kg) 45.83% (patients with PROC, active doses 1.8 mg/kg) 25.00% (1.8 mg/kg, in the NSCLC cohorts) 6.67% (2.4 mg/kg, in the NSCLC cohorts)
Patients Enrolled	Incurable, locally advanced, or metastatic disease (non-squamous NSCLC or non-mucinous PROC) that had progressed on or following prior chemotherapy and for which no standard therapy existed, Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1.
Administration Dosage	The starting dose for LIFA was 0.20 mg/kg administered by intravenous infusion (IV) every 3 weeks (Q3W), in this 3+3 dose-escalation design, followed by cohort expansion at the recommended phase II dose (RP2D).
Related Clinical Trial
NCT Number	NCT01911598	Phase Status	Phase 1a
Clinical Description	A phase 1b open-label study of the safety and pharmacokinetics of MEHD7945A in combination with either cisplatin and 5-fu or paclitaxel and carboplatin in patients with recurrent/metastatic squamous cell carcinoma of the head and neck.
Primary Endpoint	The MTD was not reached on this study and the maximum administered dose (MAD) was 2.80 mg/kg. Upon evaluation of the safety data of the 6 patients treated at the MAD, the dose of 2.40 mg/kg was established as the RP2D.
Other Endpoint	At active doses 1.80 mg/kg, partial responses were observed in four of 51 (7.84%) patients with NSCLC and 11 of 24 (45.83%) patients. In the NSCLC cohorts, PRs were seen in 1 of 4 (25.00%) at 1.80 mg/kg and in 3 of 45 (6.67%) patients at 2.40 mg/kg, mDoR=161 days. In PROC, PRs were seen at 1.80 mg/kg in one of two (50.00%), at 2.40 mg/kg in seven of 18 (38.89%), and at 2.80 mg/kg in three of four (75.00%) patients; mDoR=342 days.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[273]
Efficacy Data	Objective Response Rate (ORR)	34.00% (ITT population) 36.00% (NaPi2bx high patients)
Patients Enrolled	Advanced epithelial ovarian, primary peritoneal, or fallopian tube cancer that had progressed or relapsed within 6months of the most recent treatment with a platinum-containing chemotherapy regimen and for whom PLD was considered an appropriate therapy.
Administration Dosage	2.40 mg/kg, intravenously, every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT01991210	Phase Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer.
Primary Endpoint	The stratified PFS hazard ratio was 0.78 (95% CI,0.46-1.31; p=0.34) with a median PFS of 5.30 vs. 3.10 months (LIFA vs. PLD arm,respectively) in the ITT population, and 0.71 (95% CI,0.40-1.26; p=0.24) with a median PFS of 5.30 vs. 3.40 months (LIFA vs. PLD arm,respectively) in NaPi2bxhigh patients. The objective response rate (ORR) was 34.00% (95% CI,22.00-49.00%,LIFA) vs. 15.00% (95% CI, 7.00-28.00%,PLD) in the ITT population (p=0.03), and 36.00% (95% CI, 22.00-52.00%,LIFA) vs.14.00% (95% CI,6.00-27.00%,PLD) in NaPi2bxhigh patients (p=0.02).    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[274]
Efficacy Data	Objective Response Rate (ORR)	34.00% (all) 36.00% (SLC34A2 2+/3+)
Patients Enrolled	Platinum-resistant patients with histologically documented advanced epithelial ovarian, primary peritoneal, or fallopian tube cancer.
Administration Dosage	2.40 mg/kg, intravenously, every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT01991210	Phase Status	Phase 2
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of DNIB0600A compared to pegylated liposomal doxorubicin administered intravenously to patients with platinum-resistant ovarian cancer.
Experiment 4 Reporting the Activity Date of This ADC					[276]
Efficacy Data	Objective Response Rate (ORR)	25.00% (1.8 mg/kg NSCLC) 7.00% (2.4 mg/kg NSCLC) 50.00% (1.8 mg/kg PROC) 39.00% (2.4 mg/kg PROC) 75.00% (2.8 mg/kg PROC)
Patients Enrolled	Patients with nonsmall cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC).
Administration Dosage	Dose-escalation: 0.20-2.80 mg/kg once every 3 weeks, dose-expansion: 4 mg/kg once every 3 weeks.
Related Clinical Trial
NCT Number	NCT01363947	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DNIB0600A in patients with non-small cell lung cancer and platinum-resistant ovarian cancer.
Experiment 5 Reporting the Activity Date of This ADC					[279]
Efficacy Data	Complete Remission (CR)	58.54%
Patients Enrolled	Polycystic ovary syndrome (PSOC) patients (epithelial ovarian cancer, primary peritoneal cancer, or fallopian tube cancer) with documented radiographic progression or relapse according to RECIST v1.1.
Administration Dosage	The starting dose of LIFA was 1.20 mg/kg, once every 3 weeks (Q3W) on the first day of 21-day cycles, traditional 3 + 3 study design.
Related Clinical Trial
NCT Number	NCT01995188	Phase Status	Phase 1b
Clinical Description	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer.
Primary Endpoint	The median duration of progression-free survival was 10.71 months (95% CI: 8.54,13.86) with confirmed complete/partial responses in 24 (58.54%) patients.
Other Endpoint	The maximum tolerated dose was not reached. The recommended phase 2 dose (RP2D) was LIFA 2.40 mg/kg + carboplatin AUC6 (cycles 16), with or without bevacizumab 15 mg/kg.
Experiment 6 Reporting the Activity Date of This ADC					[282]
Related Clinical Trial
NCT Number	NCT01995188	Phase Status	Phase 1
Clinical Description	A phase 1b, open-label, dose-escalation study of the safety and pharmacology of DNIB0600A in combination with carboplatin (with or without bevacizumab) in patients with platinum-sensitive ovarian cancer or non-squamous non-small cell lung cancer.

Experiment 1 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.60% (Day 17)	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 2 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 25.40% (Day 35)	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 3 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.60% (Day 28)	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 4 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.30% (Day 62)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 5 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.70% (Day 35)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 6 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.80% (Day 28)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)

Experiment 1 Reporting the Activity Date of This ADC					[283]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.20% (Day 28)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg.    Click to Show/Hide
In Vivo Model	Ovarian adenocarcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[270]
Efficacy Data	Objective Response Rate (ORR)	2.56%	High GCC expression (GCC+++)
Patients Enrolled	Advanced or metastatic adenocarcinoma of the pancreas expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]), and previously treated with one or more prior chemotherapies.
Administration Dosage	1.80 mg/kg on day 1 of 3-week cycles as single 30-min intravenous (IV) infusions for up to 1 year or until disease progression (PD) or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02202785	Phase Status	Phase 2
Clinical Description	A phase 2 trial of mLN0264 in previously treated patients with advanced or metastatic pancreatic adenocarcinoma expressing guanylyl cyclase C (GCC).
Primary Endpoint	OrR (CR+PR)=2.56% (N=1/39), one patient achieving PR, DOR=103 days. Nine (23.07%) patients achieved SD, among those nine patients, two patients (18%, low-GCC),four patients (31%, intermediate-GCC), and three patients (20%, high-GCC).
Other Endpoint	Median OS=162 days (range 36-282) and PFS=9-82 days in the low-cohort,median OS=140 days (range 43-443) and PFS=1-218 days in the intermediate-cohort,median OS=162 days (range 49-435) and PFS=16-137 days in the high-cohort,.
Experiment 2 Reporting the Activity Date of This ADC					[271]
Efficacy Data	Objective Response Rate (ORR)	2.63%	High GCC expression (GCC+++)
Patients Enrolled	GI carcinoma expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]), included gastric carcinoma, esophageal carcinoma, colorectal carcinoma, small intestine carcinoma, pancreatic carcinoma, and biliary carcinoma.
Administration Dosage	1.80 mg/kg on day 1 of 3-week cycles as single 30-min intravenous (IV) infusions for up to 1 year or until disease progression (PD) or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02202785	Phase Status	Phase 2
Clinical Description	A phase 2 trial of mLN0264 in previously treated patients with advanced or metastatic pancreatic adenocarcinoma expressing guanylyl cyclase C (GCC).
Primary Endpoint	OrR (CR+PR)=2.63% (N=1/38), one patient identified as PR, nine patients (23.68%) had stable disease.
Experiment 3 Reporting the Activity Date of This ADC					[272]
Efficacy Data	Objective Response Rate (ORR)	5.56%	High GCC expression (GCC+++)
Patients Enrolled	Metastatic or recurrent adenocarcinoma of the stomach or gastroesophageal junction expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]) who progressed on at least one line of treatment.
Administration Dosage	TAK-264 1.80 mg/kg was administered as a 30 minute intravenous (IV) infusion on day 1 of a 21-day cycle for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02202759	Phase Status	Phase 2
Clinical Description	A phase 2 trial of mLN0264 in previously treated patients with metastatic or recurrent adenocarcinoma of the stomach or gastroesophageal junction expressing guanylyl cyclase C (GCC).
Primary Endpoint	OrR (CR+PR)=5.56% (N=2/36),2 patients achieved a PR with intermediate GCC expression.
Other Endpoint	The disease control rate (CR+PR+SD with a minimum duration of 12 weeks)=36.00%, 7 patients with high GCC expression, 4 patients with intermediate GCC expression, 4 patients with low GCC expression.
Experiment 4 Reporting the Activity Date of This ADC					[275]
Efficacy Data	Objective Response Rate (ORR)	0.00%	High GCC expression (GCC+++)
Patients Enrolled	GI carcinoma expressing GCC (H-score 10, as indicated by immunohistochemistry [IHC]), included gastric carcinoma, esophageal carcinoma, colorectal carcinoma, small intestine carcinoma, pancreatic carcinoma, and biliary carcinoma.
Administration Dosage	A conventional 3+3 dose-escalation scheme, TAK-264 doses (planned dose levels, 1.20, 1.50, 1.80, 2.10, 2.40, and 2.70 mg/kg) on day 1 of 3-week cycles as 30-minute intravenous infusions for up to 1 year or until disease progression or unacceptable toxicity.
Related Clinical Trial
NCT Number	NCT02391038	Phase Status	Phase 1
Clinical Description	A phase 1/2 trial of mLN0264 in previously treated asian patients with advanced gastrointestinal (GI) carcinoma (phase 1) or metastatic or recurrent gastric or gastroesophageal junction adenocarcinoma (phase 2) expressing guanylyl cyclase C (GCC).
Primary Endpoint	None of the patients experienced a DLT and the MTD was not determined.
Other Endpoint	There were no objective responses; three patients had stable disease.
Experiment 5 Reporting the Activity Date of This ADC					[280]
Related Clinical Trial
NCT Number	NCT02391038	Phase Status	Phase 1
Clinical Description	A phase 1/2 trial of mLN0264 in previously treated asian patients with advanced gastrointestinal (GI) carcinoma (phase 1) or Metastatic or recurrent gastric or gastroesophageal junction adenocarcinoma (phase 2) expressing guanylyl cyclase C (GCC).
Experiment 6 Reporting the Activity Date of This ADC					[281]
Patients Enrolled	GCC-expressing gastrointestinal malignancy (H-score 10, derivation described below), for whom standard treatment was no longer effective or did not offer curative or life-prolonging potential, metastatic colorectal cancer, gastric carcinoma, esophageal carcinoma, small intestine cancer, pancreatic cancer, and unknown primary malignancies.
Administration Dosage	Once every 3 weeks as a 30-minute intravenous infusion (day 1 of 21-day cycles) for up to 17 cycles or until disease progression or occurrence of unacceptable TAK-264related toxicity.
Related Clinical Trial
NCT Number	NCT01577758	Phase Status	Phase 1
Clinical Description	An open-label, dose escalation, phase 1, first-in-human study of mLN0264 in Adult patients with advanced gastrointestinal malignancies expressing guanylyl cyclase C.
Primary Endpoint	21 patients (53.85%, N=39) experienced progressive disease, 3 patients (7.69%, N=39) experienced stable disease. Median PFS=44 days (95% CI,39-83). No association between GCC expression and PFS.
Other Endpoint	MTD=1.80 mg/kg.

Experiment 1 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.00% (Day 17)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC137)
Experiment 2 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.00% (Day 28)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC129)
Experiment 3 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48.70% (Day 28)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC269)
Experiment 4 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.90% (Day 28)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC277)
Experiment 5 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.90% (Day 50)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC266)
Experiment 6 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.20% (Day 17)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC193)
Experiment 7 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.50% (Day 29)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC272)
Experiment 8 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.60% (Day 28)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC150)
Experiment 9 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.60% (Day 24)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC268)
Experiment 10 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.10% (Day 28)	High GCC expression (GCC+++)
Method Description	To evaluate the efficacy of TAK-264 in mouse models of pancreatic cancer,ten pancreatic PDX models were treated with 10 mg/kg of TAK-264 for at least 17 days. Each treatment group contained 56 mice with tumor pieces (~3mm3 fragments) injected into the right and left flank to give ~10 evaluable tumors. Mice were randomized into control or TAK-264 groups when tumor volumes reached ~150-300 mm3.    Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PANC122)

Experiment 1 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25.00 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic adenosquamous carcinoma	L3.6pl cells		CVCL_0384
Experiment 2 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25.00 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 3 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25.00 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic adenocarcinoma	Panc 03.27 cells		CVCL_1635
Experiment 4 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25.00 ug/mL	High GCC expression (GCC+++)
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic ductal adenocarcinoma	Panc 05.04 cells		CVCL_1637
Experiment 5 Reporting the Activity Date of This ADC					[284]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 25.00 ug/mL
Method Description	Anti-proliferative Effects of TAK-264 Against Pancreatic Cancer Cell Lines. Eleven pancreatic cancer cell lines were treated with TAK-264 (dose range 0.4-25 ug/mL) for 72 hours and analyzed by a SRB proliferation assay. Cell lines were deemed more responsive if proliferation was less than 50% after treatment with 25g/mL of TAK-264.
In Vitro Model	Pancreatic adenocarcinoma	Panc 02.03 cells		CVCL_1633

Experiment 1 Reporting the Activity Date of This ADC					[277]
Efficacy Data	Objective Response Rate (ORR)	36.00% (DLBCL) 50.00% (iNHL)
Patients Enrolled	Relapsed/refractory (r/r) diffuse diffuse large B-cell lymphoma (DLBCL), iNHL (including follicular lymphoma, marginal zone lymphoma, and small lymphocytic lymphoma), mantle cell lymphoma (MCL), and chronic lymphocytic leukemia (CLL), and for whom no suitable therapy of curative intent or higher priority existed.
Administration Dosage	Intravenously over 30-90 minutes in 21-day cycles, starting dose of 0.10 mg/kg.
Related Clinical Trial
NCT Number	NCT01209130	Phase Status	Phase 1
Clinical Description	An open-label, multicenter, phase 1 trial of the safety and pharmacokinetics of escalating doses of DCDT2980S in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma and chronic lymphocytic leukemia and DCDT2980S in combination with rituximab in patients with relapsed or refractory B-cell non Hodgkin's lymphoma.
Primary Endpoint	On the basis of these observations, while 3.20 mg/kg did not exceed the protocol-defined MTD.
Experiment 2 Reporting the Activity Date of This ADC					[278]
Efficacy Data	Objective Response Rate (ORR)	54.05% (R/R DLBCL, PiV% (CD22) + RTX) 66.67% (R/R FL, PiV% (CD22) + RTX)
Patients Enrolled	R/R diffuse large B-cell lymphoma (DLBCL), R/R follicular lymphoma (FL).
Administration Dosage	PiV + RTX (ADC 2.40 mg/kg + RTX 375 mg/m2) every 21 days.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	Phase 1
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of pinatuzumab vedotin (DCDT2980S) in combination with rituximab or polatuzumab vedotin (DCDS4501A) in combination with rituximab and a non-randomized phase 1b/2 evaluation of polatuzumab vedotin in combination with obinutuzumab in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma.    Click to Show/Hide
Primary Endpoint	For R/R DLBCL, ORR=51.35% (N=19/37, 95% Cl, 34.00-68.00), CR rate=13.51% (N=5/37, 95% Cl, 5.00-29.00) and PR rate=37.84% (N=14/37,95% Cl, 23.00-55.00) in patients treated with PoV (CD79b) + RTX. For R/R DLBCL, ORR=54.05% (N=20/37,95% Cl, 37.00-71.00),CR rate=18.92% (N=7/37,95% Cl, 8.00-35.00) and PR rate=35.14% (N=13/37,95% Cl, 20.00-53.00) in patients treated with PiV (CD22) + RTX.    Click to Show/Hide
Other Endpoint	For R/R FL, ORR=60.00% (N=12/20,95% Cl 36.00-81.00), CR rate=30.00% (N=6/20, 95% Cl 12.00-54.00) and PR rate=30.00% (N=6/20,95% Cl 12.00-54.00) in patients treated with PoV (CD79b) + RTX. For R/R FL, ORR=66.67% (N=14/21,95% Cl 43.00-85.00), CR rate=4.76% (N=1/21, 95% Cl 0.10-24.00) and PR rate=61.90% (N=13/21,95% Cl 38.00-52.00) in patients treated with PiV (CD22) + RTX.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Objective Response Rate (ORR)	60.00% (diffuse large B-cell lymphoma) 62.00% (follicular lymphoma cohort)
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma or relapsed or refractory grade 13a follicular lymphoma.
Administration Dosage	R-pina (375 mg/m2 rituximab plus 24 mg/kg ADCs) every 21 days until disease progression or unacceptable toxicity up to 1 year.
Related Clinical Trial
NCT Number	NCT01691898	Phase Status	Phase 1
Clinical Description	A randomized, open-label, multicenter, phase 2 trial evaluating the safety and activity of pinatuzumab vedotin (DCDT2980S) in combination with rituximab or polatuzumab vedotin (DCDS4501A) in combination with rituximab and a non-randomized phase 1b/2 evaluation of polatuzumab vedotin in combination with obinutuzumab in patients with relapsed or refractory B-cell non-Hodgkin's lymphoma.    Click to Show/Hide
Primary Endpoint	Pr=60.00%, CR=26.00% for large B-cell lymphoma. PR=62.00%,CR=70.00% for follicular lymphoma.

Experiment 1 Reporting the Activity Date of This ADC					[285]
Efficacy Data	Partial Response (PR)	4.00%
Patients Enrolled	Metastatic castration-resistant prostate cancer (CRPC).
Administration Dosage	3 + 3 dose escalation study, 0.30 to 2.80 mg/kg intravenously given once every 3 weeks followed by cohort expansion at the recommended phase II dose or weekly (0.80 to 1.00 mg/kg).
Related Clinical Trial
NCT Number	NCT01283373	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DSTP3086S in patients with metastatic castration-resistant prostate cancer.
Primary Endpoint	DsTP3086S has acceptable safety at the recommended phase II dose level of 2.40 mg/kg once every 3 weeks.
Experiment 2 Reporting the Activity Date of This ADC					[287]
Related Clinical Trial
NCT Number	NCT01283373	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study of the safety and pharmacokinetics of escalating doses of DSTP3086S in patients with metastatic castration-resistant prostate cancer.

Experiment 1 Reporting the Activity Date of This ADC					[286]
Efficacy Data	Objective Response Rate (ORR)	10.67%
Patients Enrolled	Relapsed or refractory multiple myeloma (RRMM) and Eastern Cooperative Oncology Group (ECOG) performance status of 0-2; were not eligible for stem cell/bone marrow transplant or had refused stem cell/bone marrow transplant, or had relapsed after autologous or allogeneic stem cell/bone marrow transplant.
Administration Dosage	ABBV-838 (3+3 design) intravenously starting from 0.60 mg/kg up to 6.00 mg/kg for 3-week dosing intervals (Q3W). Patients could continue ABBV-838 for up to 24 months. Assessment of alternate dosing intervals (Q1W and Q2W) was conducted in parallel.
Related Clinical Trial
NCT Number	NCT02462525	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-838, an antibody drug conjugate, in subjects with relapsed and refractory multiple myeloma.
Primary Endpoint	OrR=10.67% (N=8/75, 95% Cl 4.7-19.9), very good partial response (VGPR)=2.67% (N=2), PR=8.00% (N=6). Median DOR=4 months.
Other Endpoint	The MTD was not reached. The selected recommended dose for the expansion cohort was 5.00 mg/kg Q3W.
Experiment 2 Reporting the Activity Date of This ADC					[290]
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NCT Number	NCT02951117	Phase Status	Phase 1
Clinical Description	A phase 1b, open label, multicenter, dose escalation study of venetoclax and ABBV-838 combination therapy with dexamethasone in subjects with relapsed or refractory multiple myeloma.
Experiment 3 Reporting the Activity Date of This ADC					[291]
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NCT Number	NCT02462525	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1/1b, open-label, dose-escalation study of ABBV-838, an antibody drug conjugate, in subjects with relapsed and refractory multiple myeloma.

Experiment 1 Reporting the Activity Date of This ADC					[288]
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NCT Number	NCT01065623	Phase Status	Phase 1
Clinical Description	An open label phase 1 dose-escalation study to evaluate the safety, tolerability, pharmacokinetics, and maximum tolerated dose of BAY79-4620 administered as an intravenous infusion once every 2 weeks in patients with advanced solid tumors.
Experiment 2 Reporting the Activity Date of This ADC					[289]
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NCT Number	NCT01028755	Phase Status	Phase 1
Clinical Description	An open label phase 1 study to evaluate the safety, tolerability, pharmacokinetics and maximum tolerated dose of BAY79-4620 in patients with advanced solid tumors.