Payload Information | ADCdb

General Information of This Payload

Payload ID	PAY0IJSCK
Name	PBD dimer
Synonyms	PBD dimer; SGD-1882; 1222490-34-7; IRE1I9FE08; (6aS)-3-[3-[[(6aS)-2-methoxy-8-(4-methoxyphenyl)-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-8-(4-aminophenyl)-2-methoxy-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one; J3.194.362K; 5H-Pyrrolo(2,1-C)(1,4)benzodiazepin-5-one, 2-(4-aminophenyl)-8-(3-(((11aS)-5,11a-dihydro-7-methoxy-2-(4-methoxyphenyl)-5-oxo-1H-pyrrolo(2,1-C)(1,4)benzodiazepin-8-yl)oxy)propoxy)-1,11a-dihydro-7-methoxy-, (11aS)-; 5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one, 2-(4-aminophenyl)-8-[3-[[(11aS)-5,11a-dihydro-7-methoxy-2-(4-methoxyphenyl)-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy]propoxy]-1,11a-dihydro-7-methoxy-, (11aS)-; 8-(3-((2-(4-Aminophenyl)-7-methoxy-5-oxo-1,11abeta-dihydro-5H-pyrrolo(2,1-C)(1,4)benzodiazepine-8-yl)oxy)propoxy)-7-methoxy-2-(4-methoxyphenyl)-1,11abeta-dihydro-5H-pyrrolo(2,1-C)(1,4)benzodiazepine-5-one; 8-[3-[[2-(4-Aminophenyl)-7-methoxy-5-oxo-1,11abeta-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-8-yl]oxy]propoxy]-7-methoxy-2-(4-methoxyphenyl)-1,11abeta-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one; UNII-IRE1I9FE08; SCHEMBL2291136; OMRPLUKQNWNZAV-CONSDPRKSA-N; EX-A6227; SGD 1882; CS-7766; BP-29355; MS-31248; PD126348; HY-101127; Q27280866; (S)-2-(4-aminophenyl)-7-methoxy-8-(3-((S)-7-methoxy-2-(4-methoxyphenyl)-5-oxo-5,11a-dihydro-1H-pyrrolo[2,1-c][1,4]benzodiazepine-8-yloxy)propoxy)-1H-pyrrolo[2,1-c][1,4]benzodiazepine-5(11aH)-one; 8-(3-((2-(4-AMINOPHENYL)-7-METHOXY-5-OXO-1,11A.BETA.-DIHYDRO-5H-PYRROLO(2,1-C)(1,4)BENZODIAZEPINE-8-YL)OXY)PROPOXY)-7-METHOXY-2-(4-METHOXYPHENYL)-1,11A.BETA.-DIHYDRO-5H-PYRROLO(2,1-C)(1,4)BENZODIAZEPINE-5-ONE Click to Show/Hide
Target	Human deoxyribonucleic acid (hDNA)					Target Info
Structure
Structure	3D MOL			2D MOL
Formula	C42H39N5O7
Isosmiles	COC1=CC=C(C=C1)C2=CN3[C@@H](C2)C=NC4=CC(=C(C=C4C3=O)OC)OCCCOC5=C(C=C6C(=C5)N=C[C@@H]7CC(=CN7C6=O)C8=CC=C(C=C8)N)OC
PubChem CID	45257190
InChI	InChI=1S/C42H39N5O7/c1-50-32-11-7-26(8-12-32)28-16-31-22-45-36-20-40(38(52-3)18-34(36)42(49)47(31)24-28)54-14-4-13-53-39-19-35-33(17-37(39)51-2)41(48)46-23-27(15-30(46)21-44-35)25-5-9-29(43)10-6-25/h5-12,17-24,30-31H,4,13-16,43H2,1-3H3/t30-,31-/m0/s1
InChIKey	OMRPLUKQNWNZAV-CONSDPRKSA-N
IUPAC Name	(6aS)-3-[3-[[(6aS)-2-methoxy-8-(4-methoxyphenyl)-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-8-(4-aminophenyl)-2-methoxy-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one
Pharmaceutical Properties	Molecule Weight		725.8	Polar area		138
	Complexity		1470	xlogp Value		3.9
	Heavy Count		54	Rot Bonds		11
	Hbond acc		10	Hbond Donor		1

The activity data of This Payload

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	<0.02	mg/L	MCF-7 cells	Invasive breast carcinoma	CVCL_0031	[1]
Half Maximal Inhibitory Concentration (IC50)	<0.02	mg/L	A2780 cells	Ovarian endometrioid adenocarcinoma	CVCL_0134	[1]
Half Maximal Inhibitory Concentration (IC50)	0.08-0.16	mg/L	WI-38 cells	Normal	CVCL_0579	[1]
Half Maximal Inhibitory Concentration (IC50)	34.67	nM	Daudi cells	Burkitt lymphoma	CVCL_0008	[2]

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

ABL202 [Phase 1]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[3]
Patients Enrolled	Inclusion criteria for dose escalation: solid tumor patients (≥1 prior systemic therapy) or lymphoma patients (≥2 prior therapies per 2016 WHO criteria) with ≥1 evaluable lesion (RECIST v1.1/Lugano 2014). Dose expansion includes MCL, DLBCL (both post-≥2 therapies including BTK inhibitors), and TNBC (post-≥2 therapies), all requiring measurable lesions. Additional requirements: life expectancy >3 months, ECOG 0/1, adequate organ function, tumor tissue/blood sample provision, negative pregnancy test (females), and contraception use by all participants. Click to Show/Hide
Administration Dosage	CS5001 will be administered every 3 weeks (21 days) by intravenous (IV) infusion, and 3 weeks (21 days) is considered as one treatment cycle.
*Related Clinical Trial*
NCT Number	NCT05279300	Phase Status	PHASE1
Clinical Description	A Phase I, Dose-Escalation and Dose-Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Antitumor Activities of CS5001, an Anti-ROR1 Antibody Drug Conjugate, in Patients With Advanced Solid Tumors and Lymphomas
Primary Endpoint	The study will determine the Maximum Tolerated Dose (MTD) of CS5001 during dose escalation (over ~6 months) based on dose-limiting toxicities (DLTs) observed in participants receiving triweekly injections. The Recommended Phase 2 Dose (RP2D) will be derived from MTD data or a lower tolerable dose, incorporating safety, pharmacokinetic, pharmacodynamic, and efficacy profiles. Adverse events will be monitored for severity and incidence until 90 days post-treatment or new anticancer therapy initiation. Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis will measure concentrations of CS5001 total antibody, prodrug, free cytotoxin, and anti-CS5001 antibodies, with sampling up to 30 days after the last dose or until new anticancer therapy begins.

LCB73 [Phase 1]

ADC Info

Identified from the Human Clinical Data

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Experiment 1 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Eligible participants (≥18 years) include: Part 1 - B-cell NHL patients (excluding specific subtypes) with optional CD19 confirmation; Part 2 - confirmed CD19+ B-cell NHL (DLBCL, FL, MCL, etc.) requiring biopsy for complete response verification. All patients must have relapsed/refractory disease (≥2 prior therapies), ECOG 0-1, life expectancy ≥10 weeks, and meet contraception requirements. Part 1 allows non-measurable disease with optional biopsy; Part 2 requires measurable disease (Lugano criteria) and mandatory biopsy. Click to Show/Hide
Administration Dosage	Each patient will receive repeat doses (by intravenous (IV) infusions) on Day 1 of each 21-day cycle. Participants may continue on study until disease progression, unacceptable toxicity, or other withdrawal criteria is met.
*Related Clinical Trial*
NCT Number	NCT05365659	Phase Status	PHASE1
Clinical Description	A Phase 1 Cohort Dose Escalation and Expansion Trial to Determine the Safety, Tolerance, Maximum Tolerated Dose, and Preliminary Antineoplastic Activity of IKS03 in Patients with Advanced B Cell Non-Hodgkin Lymphomas (NHL)
Primary Endpoint	The study will determine the Recommended Dose for Expansion (RDE) in Part 1 (up to 20 months) based on DLTs and comprehensive safety data. Part 2 will assess Objective Response Rate (up to 42 months) using The Lugano Classification (Cheson 2014) for response evaluation.
Other Endpoint	Immunogenicity of IKS03 (Parts 1-2) will be evaluated through ADA measurements in serum (up to 42 months). Pharmacokinetic analysis will characterize IKS03 plasma concentrations throughout the study period. The recommended Phase 2 dose (RP2D) will be determined based on antitumor activity, tolerability, and target plasma concentration achievement (up to 42 months). Click to Show/Hide

DS-9606a [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

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Experiment 1 Reporting the Activity Date of This ADC					[5]
Patients Enrolled	Eligible participants must be ≥18 years old with ECOG 0-1, adequate organ function, and tumor tissue availability (mandatory in some cohorts). Key exclusions include active CNS metastases (unless stable post-treatment), other malignancies within 2 years (exceptions apply), significant cardiac conditions (e.g., recent MI, symptomatic CHF), QTcF >470 ms, history of interstitial lung disease, or uncontrolled infections. Contraception requirements apply throughout and post-treatment (≥6 months for males, ≥7 months for females). Dose escalation requires progressing advanced cancers (e.g., ovarian, NSCLC, gastric), while expansion focuses on ovarian cancer with mandated biopsies when feasible. Click to Show/Hide
Administration Dosage	In dose escalation, adult pts (not selected based on tumor CLDN6 expression) with ECOG PS ≤1 who progressed on/were intolerant to standard therapies, receive DS-9606a IV Q3W at 0.016-0.225 mg/kg. Primary objectives are to evaluate safety and determine the maximum tolerated dose (MTD) and recommended dose (s) for expansion (RDE).
*Related Clinical Trial*
NCT Number	NCT05394675	Phase Status	PHASE1
Clinical Description	A Phase 1, First-in-Human Study of DS-9606a in Patients With Tumor Types Known to Express Claudin-6 (CLDN6)
Primary Endpoint	The study evaluates safety through dose-limiting toxicities (DLTs) in the first two cycles (each cycle is 21 days) and treatment-emergent adverse events (TEAEs) from Cycle 1 Day 1 until 30 days post-last dose (up to 36 months). Efficacy is assessed via investigator-evaluated overall response rate (ORR) during treatment cycles, with tumor assessments every 6 weeks initially and every 12 weeks after 24 weeks. Click to Show/Hide
Other Endpoint	Pharmacokinetic parameters (AUC, Cmax, Tmax, Ctrough) will be measured across multiple timepoints during Cycles 1-4 and beyond, with assessments continuing up to 36 months. Additional efficacy endpoints include duration of response (DoR), disease control rate (DCR), time to response (TTR), progression-free survival (PFS), and immunogenicity via anti-drug antibody (ADA) evaluation at scheduled intervals. Treatment cycles follow a 21-day schedule for all assessments. Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[6]
*Related Clinical Trial*
NCT Number	NCT05394675	Phase Status	Phase 1
Clinical Description	A phase 1, first-in-human study of DS-9606a in patients with tumor types known to express claudin-6 (CLDN6).

SC-005 [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[7]
Patients Enrolled	Histologically or cytologically confirmed advanced TNBC that is relapsed, refractory, or progressive and not eligible for another standard therapy that would confer clinical benefit to the subject.
Administration Dosage	SC-005 intravenous (IV) (various doses and dose regimens)
*Related Clinical Trial*
NCT Number	NCT03316794	Phase Status	PHASE1
Clinical Description	An Open-Label Study of SC-005 in Subjects With Triple Negative Breast Cancer (TNBC)
Primary Endpoint	Number of Participants with Dose-limiting Toxicities (DLTs) [Time Frame: Minimum 21 days]
Other Endpoint	QTcF Change from Baseline [Time Frame: Up to approximately 9 weeks]; Area Under the Plasma Concentration-time Curve (AUC); Clinical benefit rate (CBR); Maximum plasma concentration observed (Cmax); Overall Survival (OS); Observed Plasma Concentrations at Trough; Duration of Clinical Benefit (DOCB)

SC-007 [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

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Experiment 1 Reporting the Activity Date of This ADC					[8]
Patients Enrolled	Eligible patients have advanced CRC (≥2 prior metastatic regimens, including pembrolizumab for MSI-H) or gastric cancer (≥2 prior lines, including HER2-targeted therapy if applicable), with ECOG 0-1 and adequate organ function. Exclusions include significant comorbidities, uninterpretable QTc, and prior exposure to PBD/indolinobenzodiazepine drugs. Click to Show/Hide
*Related Clinical Trial*
NCT Number	NCT03253185	Phase Status	PHASE1
Clinical Description	An Open Label Study of SC-007 in Subjects With Advanced Cancer
Primary Endpoint	The primary safety endpoint is the incidence of dose-limiting toxicities (DLTs) during the first treatment cycle (up to 21 days), graded per NCI CTCAE v4.03 criteria.
Other Endpoint	Key efficacy measures include clinical benefit rate (CBR=CR+PR+SD), progression-free survival (PFS), and overall survival (OS) over 4 years. Pharmacokinetic parameters (Cmax, Tmax, AUC, T1/2, Ctrough) and QTcF changes are monitored for 1 year, while anti-drug antibodies (ATAs) and objective response metrics (ORR, DOR) are tracked for 4 years.
Experiment 2 Reporting the Activity Date of This ADC					[14]
Patients Enrolled	Patients with advanced cancer (Colorectal Cancer or Gastric Cancer).
Administration Dosage	SC-007 iv.
*Related Clinical Trial*
NCT Number	NCT03253185	Phase Status	Phase 1
Clinical Description	An open label study of SC-007 in subjects with advanced cancer.

RG6148 [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[9]
Patients Enrolled	Eligible participants must have ECOG 0-1, measurable HER2+ breast cancer refractory to prior therapies, and adequate organ function. Key exclusions include recent anticancer treatments (within 4 weeks), anthracycline exposure, active infections, CNS metastases, cardiac dysfunction (LVEF <50%), QTcF >470 ms, pregnancy, or uncontrolled comorbidities. The dose-expansion cohort limits prior chemotherapy regimens to two in the metastatic setting. Click to Show/Hide
Administration Dosage	DHES0815A will be administered via intravenous (IV) infusion on Day 1 of each 21-day cycle.
*Related Clinical Trial*
NCT Number	NCT03451162	Phase Status	PHASE1
Clinical Description	A Phase I, Open-Label Study Evaluating the Safety, Tolerability, and Pharmacokinetics of Escalating Doses of DHES0815A in Patients With HER2-Positive Breast Cancer
Primary Endpoint	The study evaluates safety outcomes including adverse events (AEs) and serious AEs (SAEs) graded per NCI CTCAE v4.0 from Day 1 to study end (up to 39 months), with severity ranging from Grade 1 (mild) to Grade 5 (fatal). Dose-limiting toxicities (DLTs) are assessed during the first 21 days, including cardiac, hematologic, and hepatic events. Treatment duration and cumulative dose are tracked, along with left ventricular ejection fraction (LVEF) changes via ECHO/MUGA scans at specified intervals. Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis measures DHES0815A total antibody, conjugated PDB-MA, and unconjugated PDB-MA concentrations at multiple timepoints from Cycle 1 to study end (up to 39 months). Efficacy endpoints include objective response (CR/PR per RECIST v1.1), duration of response (DoR), and anti-drug antibody (ADA) incidence, with ADA-positive participants classified as treatment-induced or treatment-enhanced. Click to Show/Hide

SGN-CD70A [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

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Experiment 1 Reporting the Activity Date of This ADC					[10]
Patients Enrolled	Eligible patients must have metastatic renal cell carcinoma, mantle cell lymphoma, or diffuse large B-cell lymphoma (including Grade 3b follicular lymphoma) with CD70+ confirmed relapsed/refractory disease after ≥2 prior therapies, ECOG 0-1, adequate organ function, and measurable disease. Exclusions include prior anti-CD70 therapy (unless CD70+ confirmed post-treatment), recent allogeneic stem cell transplant (<100 days), or recent anticancer treatment (<4 weeks, or <2 weeks if progression occurred). Click to Show/Hide
Administration Dosage	Given intravenously every 3 weeks (or an alternate dosing schedule up to every 6 weeks)
*Related Clinical Trial*
NCT Number	NCT02216890	Phase Status	PHASE1
Clinical Description	A Phase 1 Trial of SGN-CD70A in Patients With CD70-Positive Malignancies
Primary Endpoint	The best clinical response observed at all dose levels is displayed in Table 4. One patient in the 50-ug/kg cohort achieved a partial response (PR) (6%), with a time to first response of 18.4 weeks and a response duration of ≥7.3 weeks (Fig. 1). Most patients (13 of 18; 72%) had SD, yielding an overall disease control rate of 78% (95% confidence interval, 52.4%-93.6%). Tumor size post-treatment is illustrated in Figure 2. It is noteworthy that 2 patients (1 with PR and 1 with SD) in the 50-ug/kg cohort had ongoing tumor reductions more than 6 weeks after the end of treatment (each patient had received 2 doses). Both patients experienced grade 2 thrombocytopenia, which was persistent in 1 patient. The estimated median PFS was 3.5 months (95% confidence interval, 2.1-6.3 months) (Fig. 3). Four patients are known to have died, and 14 were still alive at the last follow-up, including the patient who had a PR. The follow-up for those who remained alive at the last follow-up ranged from ≥1.4 to ≥9.7 months. Two patients who died were known to have survived for 17.6 and 14.1 months with a best response of SD. Prior immunotherapy with programmed death 1 (PD-1)/PD-L1 inhibitors was received by 4 patients (22.2%); however, the patient who attained a PR was not among them. Click to Show/Hide
Other Endpoint	Pharmacokinetic analysis measures blood concentrations of SGN-CD70A and metabolites for 3-6 weeks post-dosing, while assessing immunogenicity (antitherapeutic antibodies) and efficacy outcomes including objective response rate, progression-free survival (3-year follow-up), and duration of response (3-year follow-up).
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Objective Response Rate (ORR)	20%	Positive CD70 expression (CD70+++/++)
Patients Enrolled	CD70-positive MCL or DLBCL including FL3b (expression in at least 50% of the sample)
Administration Dosage	8 mg/kg (up to a maximum of 200 mg) intravenously once every 3 weeks.
*Related Clinical Trial*
NCT Number	NCT02216890	Phase Status	Phase 1
Clinical Description	Safety study of SGN-CD70A in cancer patients.
Primary Endpoint	Objective response rate=20.00% (95% CI 5.70-43.70).
Other Endpoint	Median progression free survival=1.90 months.

RG6109 [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[11]
Patients Enrolled	Eligible AML patients (excluding APL) must have ECOG 0-2 and adequate organ function. Arm A includes relapsed/refractory AML patients (≥18 years, ≤2 prior regimens), while Arm B enrolls treatment-naive patients (≥75 years or ≥65 years unfit for chemotherapy). Key exclusions include prior transplants, CNS leukemia, pulmonary diseases, recent investigational therapies, active infections (HCV/HBV/HIV), other recent malignancies, or QT prolongation risks. Click to Show/Hide
Administration Dosage	DCLL9718S will be administered as per the schedule specified in the respective arm.
*Related Clinical Trial*
NCT Number	NCT03298516	Phase Status	PHASE1
Clinical Description	An Open-Label, Phase I, Dose-Escalation Study Evaluating the Safety and Tolerability of DCLL9718S in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) or DCLL9718S in Combination With Azacitidine in Patients With Previously Untreated AML Unsuitable for Intensive Induction Chemotherapy
Primary Endpoint	The study evaluates safety outcomes including adverse event rates over 3 years and dose-limiting toxicities during the first treatment cycle (21-28 days depending on arm) to determine maximum tolerated dose and recommended phase 2 dose for DCLL9718S.
Other Endpoint	Pharmacokinetic parameters of DCLL9718S and azacitidine are analyzed over 3 years, including serum/plasma concentrations, AUC, Cmax, clearance, half-life, and volume of distribution. Efficacy assessments per IWG criteria measure complete remission rates (CR/CRi/CRp), overall response, duration of response, overall survival, event-free survival, progression-free survival, and anti-drug antibody development. Click to Show/Hide

SGN-CD352A [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[12]
Patients Enrolled	Eligible participants must have IMWG-defined multiple myeloma requiring systemic therapy, age ≥18 years, ECOG 0-1, life expectancy >3 months, ≥2 prior lines of therapy (including IMiD and PI), measurable disease, adequate organ function, and negative pregnancy test. Key exclusions include recent malignancies (past 3 years), active CNS disease, severe infections, HIV/HBV/HCV positivity, prior allogeneic transplant, significant pulmonary/cardiovascular comorbidities, or pregnancy/breastfeeding. Click to Show/Hide
Administration Dosage	On the first day of each 28-day cycle, SGN-CD352A will be given IV. The dose of SGN-CD352A is different in each cohort of the study, with the lowest dose in Cohort -1 (4 mcg/kg) and the highest in Cohort 6 (65 mcg/kg). Patients can only be enrolled into a higher dose level arm if lower doses have proven safe.
*Related Clinical Trial*
NCT Number	NCT02954796	Phase Status	PHASE1
Clinical Description	Phase 1 Study of SGN-CD352A in Patients With Relapsed or Refractory Multiple Myeloma
Primary Endpoint	The study assesses safety through comprehensive evaluation of adverse events (type, incidence, severity, seriousness, and relatedness) monitored for 1 month post-treatment, along with dose-limiting toxicities during the first 28-day cycle.
Other Endpoint	Efficacy outcomes include overall survival, progression-free survival, duration of response (both objective and complete), and response rates (ORR/CR) tracked for approximately 3 years, complemented by immunogenicity analysis (antitherapeutic antibodies) and pharmacokinetic profiling of SGN-CD352A and metabolites over the same period.

ABBV-322 [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.60%	Positive EGFR expression (EGFR+++/++)
Method Description	For the PDX 14R091 and PDX MPM36 studies, mice received ABBV-322 (0.03 mg/kg) or control ADC (0.03 mg/kg) every 4 days, for a total of 12 treatments.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: MPM36)
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.80%	Positive EGFR expression (EGFR+++/++)
Method Description	For the PDX 14R091 and PDX MPM36 studies, mice received ABBV-322 (0.03 mg/kg) or control ADC (0.03 mg/kg) every 4 days, for a total of 12 treatments.
In Vivo Model	Malignant Mesothelioma PDX model (PDX: 14R091)

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H2052 cells		CVCL_1518
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H2052 cells		CVCL_1518
Experiment 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural mesothelioma	NCI-H28 cells		CVCL_1555
Experiment 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 35.00 ug/mL	Positive EGFR expression (EGFR+++/++)
Method Description	Cells lines were plated at 1,000-3,000 cells per well in complete growth medium containing 10% FCS in 96-well plates and allowed to adhere overnight.
In Vitro Model	Pleural biphasic mesothelioma	MSTO-211H cells		CVCL_1430

ABT-700 (S238C)-PBD [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	70.68%	Low MET expression (MET+; IHC 1+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0363)
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	75.79%	High MET expression (MET+++; IHC 3+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0170)
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.94%	Moderate MET expression (MET++; IHC 2+)
Method Description	Tumor fragments of 3 to 5 mm at passage 3 were implanted subcutaneously in the right rear flank of NSG mice with a trochar. ABT-700 PBD was administered 0.3 mg/kg every seven days for a total of six doses.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0159)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.94%	Positive MET expression (MET +++/++)
Method Description	Mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype or ADC at 0.3 mg/kg intraperitoneally.
In Vivo Model	SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724

Revealed Based on the Cell Line Data

Click To Hide/Show 52 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1 pM	Positive MET expression (MET +++/++)
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	Anaplastic astrocytoma	DBTRG-05MG cells		CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1 pM	Positive MET expression (MET +++/++)
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	Glioblastoma	M059K cells		CVCL_0401
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1 pM	Positive MET expression (MET +++/++)
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	Glioblastoma	M059J cells		CVCL_0400
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1 pM	Positive MET expression (MET +++/++)
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	Astrocytoma	U-138MG cells		CVCL_0020
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	LS174T cells		CVCL_1384
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	SK-CO-1 cells		CVCL_0626
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.9 pM	Low MET expression (MET+)
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 adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 pM	Positive MET expression (MET +++/++)
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	Lung squamous cell carcinoma	HCC15 cells		CVCL_2057
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	DLD-1 cells		CVCL_0248
Experiment 11 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 pM	Positive MET expression (MET +++/++)
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	Gliosarcoma	SF264 cells		Homo sapiens
Experiment 12 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	SW620 cells		CVCL_0547
Experiment 13 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 pM	Positive MET expression (MET +++/++)
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 14 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 pM	Positive MET expression (MET +++/++)
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	Astrocytoma	SNB-19 cells		CVCL_0535
Experiment 15 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	SW403 cells		CVCL_0545
Experiment 16 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 7 pM	Positive MET expression (MET +++/++)
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	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 17 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 pM	Positive MET expression (MET +++/++)
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 adenocarcinoma	COLO 201 cells		CVCL_1987
Experiment 18 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	WiDr cells		CVCL_2760
Experiment 19 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
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	Rectal adenocarcinoma	SW1463 cells		CVCL_1718
Experiment 20 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive MET expression (MET +++/++)
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	RKO cells		CVCL_0504
Experiment 21 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High MET expression (MET+++)
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	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 22 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	COLO 320DM cells		CVCL_0219
Experiment 23 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	COLO 205 cells		CVCL_0218
Experiment 24 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
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	Lung squamous cell carcinoma	SW900 cells		CVCL_1731
Experiment 25 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive MET expression (MET +++/++)
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	Lung papillary adenocarcinoma	NCI-H820 cells		CVCL_1592
Experiment 26 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Low MET expression (MET+)
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	Pancreatic carcinoma	KP-4 cells		CVCL_1338
Experiment 27 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Low MET expression (MET+)
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	Glioblastoma	M059J cells		CVCL_0400
Experiment 28 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High MET expression (MET+++)
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	Gastric adenocarcinoma	Hs 746.T cells		CVCL_0333
Experiment 29 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	SW1116 cells		CVCL_0544
Experiment 30 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
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	Gliosarcoma	SF539 cells		CVCL_1691
Experiment 31 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	COLO 320HSR cells		CVCL_0220
Experiment 32 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
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	Cecum adenocarcinoma	LS1034 cells		CVCL_1382
Experiment 33 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive MET expression (MET +++/++)
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	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 34 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	LoVo cells		CVCL_0399
Experiment 35 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive MET expression (MET +++/++)
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	Lung adenocarcinoma	NCI-H1573 cells		CVCL_1478
Experiment 36 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	T84 cells		CVCL_0555
Experiment 37 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Low MET expression (MET+)
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	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 38 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Low MET expression (MET+)
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	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 39 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High MET expression (MET+++)
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	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 40 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive MET expression (MET +++/++)
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	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 41 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Low MET expression (MET+)
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	Astrocytoma	U-118MG cells		CVCL_0633
Experiment 42 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Low MET expression (MET+)
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	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 43 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive MET expression (MET +++/++)
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	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 44 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	Positive MET expression (MET +++/++)
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	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 45 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive MET expression (MET +++/++)
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	Anaplastic astrocytoma	CHLA-03-AA cells		CVCL_U616
Experiment 46 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.45 nM	Positive MET expression (MET +++/++)
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	Primitive neuroectodermal tumor	PFSK-1 cells		CVCL_1642
Experiment 47 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	SW480 cells		CVCL_0546
Experiment 48 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.2 nM	Positive MET expression (MET +++/++)
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	Glioblastoma	SNB-75 cells		CVCL_1706
Experiment 49 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67 nM	Positive MET expression (MET +++/++)
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	Glioblastoma	A-172 cells		CVCL_0131
Experiment 50 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	HCT 15 cells		CVCL_0292
Experiment 51 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 67 nM	Positive MET expression (MET +++/++)
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 adenocarcinoma	Caco-2 cells		CVCL_0025
Experiment 52 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	141 nM	Positive MET expression (MET +++/++)
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	Glioblastoma	T98G cells		CVCL_0556

D3-GPC2-PBD [Investigative]

ADC Info

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.80%	High GPC2 expression (GPC2+++)
Method Description	Tumors were typically implanted into the flanks of female 5-9 week-old C.B-17 scid mice. Each mouse was then given a single dose of their respective ADC treatments in PBS or vehicle (Day 0) via intraperitoneal (IP) injection. In some efficacy studies, one cohort of mice received 3 subsequent ADC 1 mg/kg IP injections over the following 2 weeks (1 mg/kg x 4 cohort). Click to Show/Hide
In Vivo Model	COG-N-421x PDX model

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 pM	High GPC2 expression (GPC2+++)
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	Neuroblastoma	SK-N-AS cells		CVCL_1700
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.6 pM	Positive GPC2 expression (GPC2 +++/++)
Method Description	Cell lines were plated in 96-well plates (typically between 1,000 and 5,000 cells/well) and treated with serial dilutions of each ADC payload, the D3-GPC2-PBD ADC, or vehicle the following day. After four additional days, cell viability was determined using a CellTiter-Glo Assay.
In Vitro Model	Neuroblastoma	NB-SD cells		CVCL_LF68

HuM25-S239C-PBD-E2 [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	60.13%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	EBC-1 squamous NSCLC cells (5 million) were implanted subcutaneously into SCID mice, and micewere randomized when the tumors reached 175 mm and dosed with ADC or isotype antibody at 0.6 mg/kg intraperitoneally on day 0.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	73.58%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 0.1 mg/kg intraperitoneally.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 3 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.33%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 0.3 mg/kg intraperitoneally.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 4 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	94.51%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 6 mg/kg intraperitoneally.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 pM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in LRRC15 transfected 3T12 cells by isotype-S239C-PBD-E2 or huM25-S239CPBD-E2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Squamous non-small cell lung cancer	BALB/3T12-3 cells (huLRRC15 transfection)		CVCL_0637
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 100.00 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in A549 cells that have undergone epithelial tomesenchymal transition (EMT) in the presence of 10 ng/mL TGFB by isotype-S239C-PBD-E2huM25-S239C-PBD-E2, or huM25-S239C antibody.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 100.00 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in A549 lung cancer cells in the presence of 10 ng/mL TGFB by isotype-S239C-PBD-E2huM25-S239C-PBD-E2, or huM25-S239C antibody.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Anti-ApoD PBD [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	Positive APOD expression (APOD +++/++)
Method Description	Male Bl6 mice, at 9 weeks old (young) or 80 weeks old (old), were intravenously treated with the vehicle alone or with anti-ApoD antibody and PBD-conjugated IgG with a cleavable linker, each at a concentration of 0.3 mg/kg and 3 mg/kg in a single dose.
In Vivo Model	NHDF CDX model
In Vitro Model	Normal	NHDF cells		Homo sapiens

HuAD208.4.1-PBD-DAR2 [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	EBC-1 squamous NSCLC cells (5 million) were implanted subcutaneously into SCID mice, and mice were randomized when the tumors reached 225 mm and dosed with ADC at 0.6 mg/kg Q7Dx2 (one dose given every 7 days for a total of 2 doses) or isotype antibody at 6 mg/kg intraperitoneally starting on day 0.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95.80%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	NCI-H1650 adeno NSCLCcells (5 million) were implanted subcutaneously into SCID/Beige mice, and mice were randomized whenthe tumors reached 225 mm and dosed with ADC at 0.6 mg/kg or isotype antibody at 12 mg/kg intraperitoneally once on day 0.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in murine Balb/c BM-MSC (Cyagen) mesenchymal stem cells in thepresence of 10 ng/mL TGF by isotype-PBD-DAR2 or huAD208.4.1-PBD-DAR2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Normal	Mouse bone marrow-derived mesenchymal stem (BM-MSC) cells		Mus musculus
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 - 100.00 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	In vitro cell killing in human BM-MSC (Lonza) mesenchymalstem cells in the presence of 10 ng/mL TGFB by isotype-PBD-DAR2 or huAD208.4.1-PBD-DAR2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Normal	Human bone marrow-derived mesenchymal stem (BM-MSC) cells		Homo sapiens

ZA202500202A 2188-D04-Y180-LP9 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.0003 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions. Click to Show/Hide
In Vitro Model	Embryonal carcinoma	Ntera-2 cells		CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Negative ROR1 expression (ROR1-)
Method Description	MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions. Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

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