General Information of This Payload
Payload ID
PAY0QLDVX
Name
Monomethyl auristatin F
Synonyms
MMAF; 745017-94-1; Monomethyl Auristatin F; Monomethylauristatin F; (2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid; MonomethylauristatinF; SCHEMBL3208014; CHEMBL3359822; MonoMethyl auristatin F (MMAF); MFRNYXJJRJQHNW-DEMKXPNLSA-N; DTXSID601031563; AMY30768; EX-A1046; MFCD25976742; MONOMETHYLAURISTATIN PHENYLALANINE; AC-30596; BP-22316; HY-15579; ((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)-L-phenylalanine; (2S)-2-[(2R)-2-[(R)-[(2S)-1-[(3R,4S,5S)-4-[(2S)-N,3-dimethyl-2-[(2S)-3-methyl-2-(methylamino)butanamido]butanamido]-3-methoxy-5-methylheptanoyl]pyrrolidin-2-yl](methoxy)methyl]propanamido]-3-phenylpropanoic acid; (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-Dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoic acid; ;(2~{S})-2-[[(2~{R},3~{R})-3-methoxy-3-[(2~{S})-1-[(3~{R},4~{S},5~{S})-3-methoxy-5-methyl-4-[methyl-[(2~{S})-3-methyl-2-[[(2~{S})-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methyl-propanoyl]amino]-3-phenyl-propanoic acid; L-PHENYLALANINE, N-METHYL-L-VALYL-L-VALYL-(3R,4S,5S)-3-METHOXY-5-METHYL-4-(METHYLAMINO)HEPTANOYL-(.ALPHA.R,.BETA.R,2S)-.BETA.-METHOXY-.ALPHA.-METHYL-2-PYRROLIDINEPROPANOYL-
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Target(s) Microtubule (MT)
Structure
Formula
C39H65N5O8
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](CC2=CC=CC=C2)C(=O)O)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC
PubChem CID
10395173
InChI
InChI=1S/C39H65N5O8/c1-12-25(6)34(43(9)38(48)33(24(4)5)42-37(47)32(40-8)23(2)3)30(51-10)22-31(45)44-20-16-19-29(44)35(52-11)26(7)36(46)41-28(39(49)50)21-27-17-14-13-15-18-27/h13-15,17-18,23-26,28-30,32-35,40H,12,16,19-22H2,1-11H3,(H,41,46)(H,42,47)(H,49,50)/t25-,26+,28-,29-,30+,32-,33-,34-,35+/m0/s1
InChIKey
MFRNYXJJRJQHNW-DEMKXPNLSA-N
IUPAC Name
(2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid
Pharmaceutical Properties
Molecule Weight
732
Polar area
167
Complexity
1160
xlogp Value
2.1
Heavy Count
52
Rot Bonds
21
Hbond acc
9
Hbond Donor
4
The activity data of This Payload
Standard Type Value Units Cell line Disease Model Cell line ID Reference
Half Maximal Inhibitory Concentration (IC50) 10 nM
HT-29 cells
Colon adenocarcinoma
CVCL_0320 
[1]
Half Maximal Inhibitory Concentration (IC50) 105 nM
H3396 cells
Breast carcinoma
CVCL_D348 
[1]
Half Maximal Inhibitory Concentration (IC50) 137 nM
HL-60 cells
Adult acute myeloid leukemia
CVCL_0002 
[1]
Half Maximal Inhibitory Concentration (IC50) 2880 nM
HCT 116 cells
Colon carcinoma
CVCL_0291 
[1]
Half Maximal Inhibitory Concentration (IC50) 5.3 nM
SK-BR-3 cells
Breast adenocarcinoma
CVCL_0033 
[2]
Half Maximal Inhibitory Concentration (IC50) 7 nM
Hep-G2 cells
Hepatoblastoma
CVCL_0027 
[3]
Half Maximal Inhibitory Concentration (IC50) 8.8 nM
BT474-M1 cells
Invasive breast carcinoma
CVCL_0179 
[2]
Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
Belantamab mafodotin [Approved]
Identified from the Human Clinical Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [4]
Efficacy Data Objective Response Rate (ORR)
60.00%
Patients Enrolled
Histologically or cytologically confirmed MM, a European Cooperative Oncology Group performance status of 0 or 1, prior therapy with alkylators, PI and IMiD, had undergone stem cell transplant (if eligible) and refractory to the last line of treatment (defined as progressive disease on or within 60 days of completion of the last therapy) that included stem cell transplant and those patients with a history of autologous stem cell transplant must have received the transplant >100 days prior to study enrolment and have no active infection.

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Administration Dosage
Doses ranging between 0.03 mg/kg and 4.60 mg/kg was administered as a 1-hour intravenous infusion every 3 weeks for a maximum of 16 cycles.
Related Clinical Trial
NCT Number NCT02064387  Phase Status Phase 1
Clinical Description
A phase 1 open-label, dose escalation study to investigate the safety, pharmacokinetics, pharmacodynamics, immunogenicity and clinical activity of the antibody drug conjugate GSK2857916 in subjects with relapsed/refractory multiple myeloma and other advanced hematologic malignancies expressing BCMA.
Primary Endpoint
The primary endpoints of the trial were to determine the safety, tolerability, maximum tolerated dose (MTD) and RP2D and schedule of GSK2857916. Median PFS (post hoc analysis) was 7.90 months (95% CI: 3.1-not estimable),Overall response rate at 3.40 mg/kg in Part 2 was 60.00% (21/35; 95% confidence interval: 42.10%-76.10%).
Other Endpoint
PK profile (single dose area under the curve, maximum serum concentration [Cmax], time to Cmax , clearance, steady-state volume of distribution [Vss], half-life [t]; repeat dose Cmax and trough plasma concentration), the incidence of anti-drug antibodies, and clinical activity measured as overall response rate (ORR), defined as the percentage of subjects achieving confirmed partial response or better (PR) and clinical benefit rate, defined as the percentages of subjects with minimal response or better (MR).

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Experiment 2 Reporting the Activity Date of This ADC [5]
Efficacy Data Objective Response Rate (ORR)
60.00%
High BCMA expression (BCMA +++)
Patients Enrolled
Eligible adult (18 years of age) patients for part 2 had histologically or cytologically confirmed MM, Eastern Cooperative Oncology Group performance status 0 or 1, prior therapy with alkylators, proteasome inhibitors and immunomodulators, and were refractory to the last line of treatment.
Administration Dosage
GSK2857916 3.4 mg/kg was administered through 1-h intravenous infusions once every 3 weeks, for a maximum of 16 cycles.
Related Clinical Trial
NCT Number NCT02064387   Phase Status Phase 1
Clinical Description
A Phase I open-label, dose escalation study to investigate the safety, pharmacokinetics, pharmacodynamics, immunogenicity and clinical activity of the antibody drug conjugate GSK2857916 in subjects with relapsed/refractory multiple myeloma and other advanced hematologic malignancies expressing BCMA.
Primary Endpoint
Objective response rate=60.00% (95% CI 42.10-76.10), comprising 5 (14.29%) achieving complete responses and 16 (45.71%) achieving partial responses.
Other Endpoint
The median progression-free survival was 12.00 months and the median duration of response was 14.30 months.
Experiment 3 Reporting the Activity Date of This ADC [6]
Related Clinical Trial
NCT Number NCT03769506  Phase Status Phase 3
Clinical Description
A phase 3, randomized, double-arm, open-label, controlled trial of ASP-1929 photoimmunotherapy versus physician's choice standard of care for the treatment of locoregional, recurrent head and neck squamous cell carcinoma in patients who have failed or progressed on or after at least two lines of therapy, of which at least one line must be systemic therapy.

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Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [7]
Efficacy Data Half Maximal Effective Concentration (EC50)
30.60 ug/mL
Moderate BCMA expression (BCMA++)
Method Description
Cells (5 x 105 cells/mL) were left untreated or exposed to the indicated treatments for the indicated time. Cells were counted on a Vi-Cell-XR Cell Viability Analyzer (Beckman Coulter).
In Vitro Model Thymoma EL4 cells (BCMA expression) CVCL_0255
ARX-788 [Phase 3]
Identified from the Human Clinical Data
Click To Hide/Show 12 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [8]
Efficacy Data Objective Response Rate (ORR)
57.10%
Patients Enrolled
Patients with HER2+ mBC whose disease has progressed following T-DM1, T-DXd, and/or tucatinib-containing regimens.
Administration Dosage
Administered with an initial dose of 1.50 mg/kg Q4W and subsequent doses of 1.30 mg/kg Q4W.
Related Clinical Trial
NCT Number NCT04829604  Phase Status Phase 2
Clinical Description
A global, phase 2 study of ARX788 in HER2-positive metastatic breast cancer patients who were previously treated with T-DXd.
Experiment 2 Reporting the Activity Date of This ADC [9]
Efficacy Data Objective Response Rate (ORR)
33.30% (1.3 mg/kg)
46.20% (1.5 mg/kg)
28.60% (1.7 mg/kg)
Patients Enrolled
Twenty-two (73.30%) had gastric adenocarcinoma, and the rest (26.70%) had GEJ adenocarcinoma.
Administration Dosage
At least one dose of ARX788, of whom 9 patients received 1.30 mg/kg, 14 received 1.50 mg/kg, and 7 received 1.70 mg/kg ARX788. The median treatment duration was 3.5 (range: 1-29) cycles.
Related Clinical Trial
NCT Number CTR20171162  Phase Status Phase 1
Clinical Description
A phase 1 study of ACE-Breast-01 [ZMC-ARX788111 (CTR20171162)] to test the safety, PK, and antitumor activity of ARX788 in patients in China with HER2-positive metastatic breast cancer (MBC) whose disease had progressed on prior anti-HER2 treatments. The study includes dose escalation(N=69) to determine the maximum tolerated dose (MTD)/recommended phase 2 dose (RP2D) in patients with HER2-positive MBC.

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Primary Endpoint
The MTD of ARX788 was not reached at doses of up to 1.50 mg/kg every 3 weeks. the RP2D in breast cancer studies was determined to be 1.50 mg/kg every 3 weeks. 33 of the 69 (47.83%) patients had an objective partial tumor response. For ARX788 1.50 mg/kg every 3 weeks, the objective response rate was 65.52% [19/29, 95% confidence interval (CI), 45.70-82.10], the disease control rate was 100.00% (95% CI, 81.20-100.00), and the median progression-free survival was 17.02 months (95% CI, 10.09-not reached).

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Experiment 3 Reporting the Activity Date of This ADC [9]
Efficacy Data Objective Response Rate (ORR)
37.90%
Patients Enrolled
HER2-positive advanced gastric/gastroesophageal junction adenocarcinoma failing to respond to prior trastuzumab-based standard treatment, at least one dose.
Administration Dosage
9 patients received 1.30 mg/kg, 14 received 1.50 mg/kg, and 7 received 1.70 mg/kg ARX788.
Related Clinical Trial
NCT Number CTR20171162  Phase Status Phase 1
Clinical Description
A phase 1 study in HER2-positive advanced ug/GEJ adenocarcinoma was initiated to evaluate the safety and efficacy of ARX788. There were 22 males (73.3%) and 8 females (26.7%). Twenty-two (73.3%) had gastric adenocarcinoma,and the rest (26.7%) had GEJ adenocarcinoma. Twenty-seven patients (90%) underwent prior trastuzumab-containing therapy,eight of whom progressed within 6 months in the adjuvant or neoadjuvant phase. Twelve (40%) were treated with 2 or more lines of therapy (26) and eight of whom had 3 or more lines. All patients were treated with platinum-based and fluorouracil regimens,and eight with taxanes and three with irinotecan. Most participants (73.3%) had an Eastern Cooperative Oncology Group (ECOG) performance status (PS) of 1. All of them had at least one dose of ARX788,of whom 9 patients received 1.3 mg/kg,14 received 1.5 mg/kg,and 7 received 1.7 mg/kg ARX788.

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Primary Endpoint
For ARX788 1.70 mg/kg, a median follow up of 10 (95% CI: 6.50-15.90) months,the median PFS was 4.10 (95% CI,1.40-6.40) months,and the median OS was 10.70 (95% CI,4.80-not reached) months.
Experiment 4 Reporting the Activity Date of This ADC [10]
Efficacy Data Objective Response Rate (ORR)
65.52%
Patients Enrolled
Incurable, locally advanced, or metastatic HER2-positive (immunohistochemistry [IHC] 3+ and/or fluorescence in situ 1 hybridization [FISH]-positive) breast cancer that progressed on greater and or 2 equal to two prior anti-HER2 treatment(s) in the advanced disease setting and 3 who provided written informed consent, patients had an Eastern 4 Cooperative Oncology Group (ECOG) performance status of 0-1.

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Administration Dosage
0.33 mg/kg Q3W, 0.66 mg/kg Q3W, 0.88 mg/kg Q4W, 0.88 mg/kg Q3W, 1.10 mg/kg Q4W, 1.10 mg/kg Q3W, 1.30 mg/kg Q4W, 1.30 mg/kg Q3W, and 1.50 mg/kg Q3W, intravenous infusion.
Related Clinical Trial
NCT Number CTR20171162  Phase Status Phase 1
Clinical Description
Patients with HER2-positive MBC received ARX788 at doses of 0.33, 0.66, 0.88, 1.10, 1.30, or 1.50 mg/kg every 3 weeks, or 0.88, 1.10, or 1.30 mg/kg every 4 weeks. The dose-limiting toxicity (DLT) was assessed for 84 days for pulmonary toxicity and at a duration of one cycle (21 or 28 days) for other toxicities. In total, 69 patients were enrolled. No DLT or drug-related deaths occurred.

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Primary Endpoint
At 1.50 mg/kg every 3 weeks, the recommended phase II dose, the objective response rate was 65.52% [19/29, 95% confidence interval (CI), 45.70-82.10].
Other Endpoint
The disease control rate was 100.00% (95% CI, 81.20-100.00), and the median progression-free survival was 17.02 months (95% CI, 10.09-not reached).
Experiment 5 Reporting the Activity Date of This ADC [11]
Efficacy Data Objective Response Rate (ORR)
74.00% (Breast cancer)
67.00% (Pan-tumor)
Patients Enrolled
ACE-Breast-01 (median 6 prior lines of therapy) and ACE-Pan tumor-01 trial (including breast, gastric/GEJ, NSCLC, ovarian, urothelial, biliary track, endometrial, and salivary gland cancer).
Administration Dosage
0.33 - 1.5 mg/kg; Q3W or Q4W.
Related Clinical Trial
NCT Number NCT03255070  Phase Status Phase 1
Clinical Description
A phase 1, multicenter, open-label, multiple dose-escalation and expansion study of ARX788, as monotherapy in advanced solid tumors with HER2 expression.
Experiment 6 Reporting the Activity Date of This ADC [14]
Related Clinical Trial
NCT Number NCT05426486  Phase Status Phase 2/3
Clinical Description
A randomized, open label, multi-center phase 2-2i neoadjuvant study comparing the efficacy and safety of ARX788 combined with pyrotinib maleate versus TCBHP (trastuzumab plus pertuzumab with docetaxel and carboplatin) in patients with HER2-positive breast cancer.
Experiment 7 Reporting the Activity Date of This ADC [15]
Related Clinical Trial
NCT Number NCT05041972  Phase Status Phase 2
Clinical Description
A global phase 2 study to evaluate the efficacy and safety of ARX788 for selected HER2-mutated or HER2-amplified/overexpressed solid tumors.
Experiment 8 Reporting the Activity Date of This ADC [16]
Related Clinical Trial
NCT Number NCT05018702  Phase Status Phase 2
Clinical Description
A prospective, single-arm, single-center phase 2 clinical study of recombinant humanized anti-HER2 monoclonal antibody-AS269 conjugate (ARX788) in the treatment of HER2-positive breast cancer patients with brain metastases.
Experiment 9 Reporting the Activity Date of This ADC [17]
Related Clinical Trial
NCT Number NCT05018676  Phase Status Phase 2
Clinical Description
A single-arm, single-center phase 2 clinical study of recombinant humanized anti-HER2 monoclonal antibody-AS269 conjugate (ARX788) in the treatment of unresectable and/or metastatic breast cancer with low expression of HER2.
Experiment 10 Reporting the Activity Date of This ADC [18]
Related Clinical Trial
NCT Number NCT04983121  Phase Status Phase 2
Clinical Description
Efficacy and safety of pyrotinib maleate combined with ARX788 neoadjuvant treatment in stage 2-2I HER2-positive breast cancer patients who have poor outcomes after treatment with trastuzumab and pertuzumab.
Experiment 11 Reporting the Activity Date of This ADC [19]
Related Clinical Trial
NCT Number NCT01042379  Phase Status Phase 2
Clinical Description
I-SPY trial (investigation of serial studies to predict your therapeutic response with imaging and molecular analysis 2).
Experiment 12 Reporting the Activity Date of This ADC [20]
Related Clinical Trial
NCT Number NCT02512237  Phase Status Phase 1
Clinical Description
A phase 1, multicenter, open-label, multiple dose-escalation study of ARX788, intravenously administered as a single agent in subjects with advanced cancers with HER2 expression.
LCB14-0110 [Phase 3]
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]
Efficacy Data Objective Response Rate (ORR)
66.70% (> 1.00 mg/kg)
42.90% (HER2-Low)
Patients Enrolled
Patients with HER2-expresssing advanced solid tumors who had failed prior standard of care therapies.
Administration Dosage
FS-1502 was given IV once in 21-day or 28-day cycle at doses of 0.10-3.50 mg/kg.
Depatuxizumab mafodotin [Phase 3]
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [13]
Efficacy Data Median progression-free survival (mPFS)
8.00 (depatux-m group); 6.30 (placebo group)
High EGFR expression (EGFR +++)
Patients Enrolled
EGFR-amp newly diagnosed GBM were randomized 1:1 to radiotherapy, temozolomide, and depatux-m/placebo.
Administration Dosage
Depatux-m was dosed at 2.0 mg/kg during RT, then 1.25 mg/kg thereafter on days 1 and 15/28, 19,21 and allowed to continue until disease progression.
Experiment 2 Reporting the Activity Date of This ADC [13]
Efficacy Data Median Overall Survival (mOS)
18.90 (depatux-m group); 18.70(placebo group)
High EGFR expression (EGFR +++)
Patients Enrolled
EGFR-amp newly diagnosed GBM were randomized 1:1 to radiotherapy, temozolomide, and depatux-m/placebo.
Administration Dosage
Depatux-m was dosed at 2.0 mg/kg during RT, then 1.25 mg/kg thereafter on days 1 and 15/2819, 21 and allowed to continue until disease progression.
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [21]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.50% (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 [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ug/mL - 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
Experiment 3 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ug/mL - 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 [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ug/mL - 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 5 Reporting the Activity Date of This ADC [21]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ug/mL - 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
GPC-1-ADC [Investigative]
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 [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 22.63% (Day 28) Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (1 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model Pancreatic cancer PDX model
Experiment 2 Reporting the Activity Date of This ADC [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 29.66% (Day 28) Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (3 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model Pancreatic cancer PDX model
Experiment 3 Reporting the Activity Date of This ADC [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.22% (Day 28) Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (10 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model Pancreatic cancer PDX model
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.97% (Day 36) Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour-bearing mice were intravenously administered PBS, control ADC or GPC-1-ADC (1 mg/kg) on days 0, 4, 8 and 12.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.00% (Day 36) Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour-bearing mice were intravenously administered PBS, control ADC or GPC-1-ADC (3 mg/kg) on days 0, 4, 8 and 12.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC [22]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.00% (Day 36) Positive GPC-1 expression (GPC-1 +++/++)
Method Description
Tumour-bearing mice were intravenously administered PBS, control ADC (10 mg/kg ) or GPC-1-ADC (10 mg/kg) on days 0, 4, 8 and 12, once every 4 days for a total of four doses.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
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 [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 nM
Positive GPC-1 expression (GPC-1 +++/++)
Method Description
IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.24 nM
Positive GPC-1 expression (GPC-1 +++/++)
Method Description
IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model Pancreatic ductal adenocarcinoma T3M-4 cells CVCL_4056
Experiment 3 Reporting the Activity Date of This ADC [22]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative GPC-1 expression (GPC-1 -)
Method Description
IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model Pancreatic ductal adenocarcinoma SUIT-2 cells CVCL_3172
ASG-15MF [Investigative]
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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 62.90% (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,ASG-15MF 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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 63.40% (Day 25) High SLITRK6 expression (SLITRK6+++; IHC H-score=230)
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,ASG-15MF 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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.00% (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,ASG-15MF 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)
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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.20% (Day 21) Moderate SLITRK6 expression (SLITRK6++; IHC H-score=185)
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. ASG-15MF was administered twice weekly at 3 mg/kg (n = 6) starting when the tumor volume reached approximately 200 mm3.
In Vivo Model NCI-322M CDX model
In Vitro Model Lung cancer NCI-322M cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.30% (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 ASG-15MF, 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
HuM25-mcMMAF-E2 [Investigative]
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 [24]
Efficacy Data Tumor Growth Inhibition value (TGI)
0.00%
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-MCMMAF-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 2 Reporting the Activity Date of This ADC [24]
Efficacy Data Tumor Growth Inhibition value (TGI)
8.47% (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-MCMMAF-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
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [24]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 nM - 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
GPC-1 ADC 1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [25]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 21.71% (Day 24) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (1 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC [25]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 28.13% (Day 32) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (1 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 3 Reporting the Activity Date of This ADC [25]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 33.65% (Day 32) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (3 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 4 Reporting the Activity Date of This ADC [25]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 43.94% (Day 24) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (3 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 5 Reporting the Activity Date of This ADC [25]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.65% (Day 24) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (10 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 6 Reporting the Activity Date of This ADC [25]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.49% (Day 32) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (10 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
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 [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Positive GPC1 expression (GPC1 +++/++)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 nM
Positive GPC1 expression (GPC1 +++/++)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 3 Reporting the Activity Date of This ADC [25]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative GPC1 expression (GPC1 -)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Ovarian clear cell adenocarcinoma RMG-I cells CVCL_1662
Anti-BCMA J6M0-mcMMAF [Investigative]
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 [26]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 24.38% (Day 21) High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model NCI-H929 CDX model
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC [26]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 65.09% (Day 32) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1S CDX model
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [26]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 66.25% (Day 21) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
Experiment 4 Reporting the Activity Date of This ADC [26]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.86% (Day 35) High BCMA expression (BCMA+++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 3 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model MM.1R CDX model
In Vitro Model Plasma cell myeloma MM1.R cells CVCL_8794
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 [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
29.28 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
55.55 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
159.70 nM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC [26]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.46 uM
Moderate BCMA expression (BCMA++)
Method Description
The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Ab3-mcMMAF [Investigative]
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 [27]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.23% (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
HA15-1C25F [Investigative]
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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 35.90% (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 Ha15-1c25F, 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
HA15-1ABE16F [Investigative]
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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 44.70% (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 Ha15-1abe16F, 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
WO2017089890A1 ADC34 [Investigative]
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 [28]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.68% (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 [28]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.39% (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
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Ch14.18-MMAF [Investigative]
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 [29]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.74% (Day 44) 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 EL-4 CDX model
In Vitro Model Thymoma EL4 cells CVCL_0255
Experiment 2 Reporting the Activity Date of This ADC [29]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 74.95% (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
Revealed Based on the Cell Line Data
Click To Hide/Show 38 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 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 2 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 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 3 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.81 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 4 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.27 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 5 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.84 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 6 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.30 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 7 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.70 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 8 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.80 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 [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 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 Astrocytoma 1321N1 cells CVCL_0110
Experiment 10 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
18.00 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 11 Reporting the Activity Date of This ADC [29]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 20.00 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 Osteosarcoma MG-63 cells CVCL_0426
Experiment 12 Reporting the Activity Date of This ADC [29]
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 Bone marrow neuroblastoma SH-SY5Y cells CVCL_0019
Experiment 13 Reporting the Activity Date of This ADC [29]
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 14 Reporting the Activity Date of This ADC [29]
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 15 Reporting the Activity Date of This ADC [29]
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 16 Reporting the Activity Date of This ADC [29]
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 17 Reporting the Activity Date of This ADC [29]
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 Amelanotic melanoma A375 cells CVCL_0132
Experiment 18 Reporting the Activity Date of This ADC [29]
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 [29]
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 [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.02 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 21 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.02 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 22 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.19 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 23 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.25 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 24 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.30 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 25 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
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 Amelanotic melanoma COLO 38 cells CVCL_3934
Experiment 26 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.30 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 27 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
0.48 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 [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
1.00 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 Astrocytoma 1321N1 cells CVCL_0110
Experiment 29 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
5.30 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 [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
5.30 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 31 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
5.30 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 32 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
7.30 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 33 Reporting the Activity Date of This ADC [29]
Efficacy Data 20% Maximal Inhibitory Concentration (IC20)
12.40 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 Glioblastoma U-87MG cells CVCL_0022
Experiment 34 Reporting the Activity Date of This ADC [29]
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 35 Reporting the Activity Date of This ADC [29]
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 36 Reporting the Activity Date of This ADC [29]
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 37 Reporting the Activity Date of This ADC [29]
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 Melanoma B16 cells CVCL_F936
Experiment 38 Reporting the Activity Date of This ADC [29]
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
RBGO1-mcF [Investigative]
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 [30]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 60.00% (Day 20) Positive RAGE expression (RAGE+++/++)
Method Description
Nude athymic mice were divided into three treatment groups of six mice each. Mice were treated with PBS (control) or RBGO1 ADC at either 3 mg/kg or 20mg/kg N intravenous injection. Bodyweight was measured at days 3, 6, 8, 13, 17 and 21 and mouse health assessed daily.
In Vivo Model HEC-1-A CDX model
In Vitro Model Endometrial adenocarcinoma HEC-1-A cells CVCL_0293
M25ADCMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [31]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 62.30% (Day 31) Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 150 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for a total of 4 doses at 5 mg/kg.
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 [31]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.16% (Day 32) 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 a total of 4 doses at 5 mg/kg.
In Vivo Model M28 CDX model
In Vitro Model Pleural malignant mesothelioma M28K cells CVCL_8106
Experiment 3 Reporting the Activity Date of This ADC [31]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.72% (Day 37) Positive ALPPL2 expression (ALPPL2+++/++)
Method Description
Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 500 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for a total of 4 doses at 5 mg/kg.
In Vivo Model M28 CDX model
In Vitro Model Pleural malignant mesothelioma M28K cells CVCL_8106
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [31]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.40 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 [31]
Efficacy Data Half Maximal Effective Concentration (EC50)
36.00 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 [31]
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 [31]
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 [31]
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
HA15-10AC14F [Investigative]
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 [23]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 64.30% (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 Ha15-10ac14F, 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
GPC1-ADC-MMAF [Investigative]
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 [32]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.70% (Day 28) High GPC1 expression (GPC1+++)
Method Description
The SCID mice were subcutaneously inoculated with BxPC-3-GPC1-KO-Luc#15 cells and then intravenously treated with PBS, 10-mg/kg control-ADC, or 10-mg/kg humanized GPC1-ADC(MMAE) twice a week for a total of four times.
In Vivo Model BxPC-3 CDX model
In Vitro Model Pancreatic ductal adenocarcinoma BxPC-3 cells CVCL_0186
h1F6-mcMMAF [Investigative]
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 [33]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 76.44% (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 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.21% (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
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 [33]
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 2 Reporting the Activity Date of This ADC [33]
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 Renal cell carcinoma 786-O cells CVCL_1051
hBU12-mcMMAF [Investigative]
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 [33]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 76.44% (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 2 Reporting the Activity Date of This ADC [33]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.21% (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
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 [33]
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 2 Reporting the Activity Date of This ADC [33]
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 Renal cell carcinoma 786-O cells CVCL_1051
LCB14-0648 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [34]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 80.97% (Day 21) Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 2 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC [34]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.16% (Day 21) Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 5 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC [34]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 88.70% (Day 21) Positive CD19 expression (CD19 +++/++)
Method Description
6-week old female irradiated Balb/c nude mice were subcutaneously injected with 5x106 Ramos cells. After two weeks, tumor volume reached about 130 mm, and micewere randomly divided into groups of 10. Mice were then injected intravenously with 10 mg/kg of ADC or unconjugated antibody or vehicle (PBS).
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
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 [34]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110 ng/mL
Positive CD19 expression (CD19 +++/++)
Method Description
Raji cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 ug/mL Negative CD19 expression (CD19 -)
Method Description
K562 cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°Cin 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
Ab1-mcMMAF [Investigative]
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 [27]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 81.39% (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 2 Reporting the Activity Date of This ADC [27]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.40% (Day 55) 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
IC1-MMAF [Investigative]
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 [35]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.30% (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 2 Reporting the Activity Date of This ADC [35]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.00% (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
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 [35]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.30 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 [35]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
68.70 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 Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [35]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.12 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
1F6-Val-Cit-PABC-MMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [36]
Efficacy Data Tumor Growth Inhibition value (TGI)
84.59% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model DBTRG-05MG glioblastoma cell line xenograft model
In Vitro Model Anaplastic astrocytoma DBTRG-05MG cells CVCL_1169
Experiment 2 Reporting the Activity Date of This ADC [36]
Efficacy Data Tumor Growth Inhibition value (TGI)
85.01% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
1 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [36]
Efficacy Data Tumor Growth Inhibition value (TGI)
93.25% (Day 30)
Positive TNF expression (TNF+++/++)
Method Description
3 mg mAb component/kg in vivo therapeutic efficacy of the conjugates in nude mice(5 animals/group).
In Vivo Model 786-O human RCC cell line xenograft model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.90±2.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 2 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.10±2.70 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.10±3.60 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
WO2007011968A2 c1F6-9b [Investigative]
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [37]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.08% (Day 41) Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
An in vivo therapy experiments with c1F6-9b was undertaken in nude mice with subcutaneous 786-O cells. The animals (5 per group)were treated with a single intravenous dose of c1F6-9b at 0.75 mg/kg (mAb component) on day 14.
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 [37]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 89.93% (Day 41) Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
An in vivo therapy experiments with c1F6-9b was undertaken in nude mice with subcutaneous 786-O cells. The animals (5 per group)were treated with a single intravenous dose of c1F6-9b at 1.5 mg/kg (mAb component) on day 14.
In Vivo Model 786-O CDX model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [37]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 94.00% (Day 41) Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description
An in vivo therapy experiments with c1F6-9b was undertaken in nude mice with subcutaneous 786-O cells. The animals (5 per group)were treated with a single intravenous dose of c1F6-9b at 3 mg/kg (mAb component) on day 14.
In Vivo Model 786-O CDX model
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
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 [37]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.08 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 [37]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 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 [37]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 50.00 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
Anti-BCMA 15B2WT-mcMMAF [Investigative]
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 [26]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.16% (Day 21) Moderate BCMA expression (BCMA++)
Method Description
Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model JJN-3 CDX model
In Vitro Model Plasma cell myeloma JJN-3 cells CVCL_2078
WO2017089890A1 ADC23 [Investigative]
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 [28]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 96.52% (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 [28]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.72% (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
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.44 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.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
HER2-acetal-ADC 12 [Investigative]
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 [38]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 30) Positive HER2 expression (HER2 +++/++)
Method Description
NOD-SCID mice with heterotopic SKBR-3 tumor xenografts were injected intravenously with either ADC 12 (1.12 mg/kg; group A), PBS 1x (vehicle; group B) or Kadcyla (1.12 mg/kg; group C) and tumor volume was measured every 2-3 days for 30 days.
In Vivo Model SKBR-3 CDX model
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
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 [38]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.22 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 [38]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative 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 MDA-MB-231 cells CVCL_0062
EVCit ADC 3c [Investigative]
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 [39]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 18) Positive HER2 expression (HER2+++/++)
Method Description
EVCit ADC 3c (3 mg/kg, single dose) induces efficient tumor cell killing in cell line-derived models of KPL-4 cells with HER2 expression with high expression.
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
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 [39]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM-0.12 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 2 Reporting the Activity Date of This ADC [39]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2-)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
VCit ADC 3a [Investigative]
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 [39]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 18) Positive HER2 expression (HER2+++/++)
Method Description
VCit ADC 3a (3 mg/kg, single dose) induces efficient tumor cell killing in cell line-derived models of KPL-4 cells with HER2 expression with high expression.
In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
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 [39]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.10 nM-0.12 nM
Positive HER2 expression (HER2+++/++)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 2 Reporting the Activity Date of This ADC [39]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative HER2 expression (HER2-)
Method Description
Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
hBU12-mc-MMAF [Investigative]
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 [40]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 13) Positive CD19 expression (CD19 +++/++)
Method Description
We tested the activity of anti-human CD19-targeted ADCs in a human CD19+ Ramos non-Hodgkin lymphoma xenograft tumor model.
In Vivo Model Ramos CDX model
In Vitro Model Burkitt lymphoma Ramos cells CVCL_0597
WO2017089895A1 ADC34 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
58.23% (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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
87.94% (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
Revealed Based on the Cell Line Data
Click To Hide/Show 7 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 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 [41]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [41]
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 were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC23 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
96.08% (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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
99.23% (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
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 [41]
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 3 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.21 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.44 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.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC [41]
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 were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Trastuzumab DVD-ADC [Investigative]
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 [42]
Efficacy Data Inhibition rate (100nM)
0.00%
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [42]
Efficacy Data Inhibition rate (100nM)
0.00%
High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [42]
Efficacy Data Inhibition rate (100nM) > 50.00% High HER2 expression (HER2+++); Moderate TRKB expression (TRKB++)
Method Description
Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
ZHER2-ABD-mcMMAF [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 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 Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 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 3 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.20 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 AU565 cells CVCL_1074
Experiment 4 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
12.00 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 Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [43]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
215 nM
Moderate 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 Lung adenocarcinoma A-549 cells CVCL_0023
WO2017089895A1 ADC77 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [41]
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 were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC62 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 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 [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC [41]
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 were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 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 [41]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC40 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 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 [28]
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
WO2017089890A1 ADC77 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.02 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 [28]
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
WO2017089895A1 ADC53 [Investigative]
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 [41]
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 [41]
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 [41]
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
WO2017089895A1 ADC50 [Investigative]
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 [41]
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 [41]
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 [41]
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
WO2017089895A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 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 [41]
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 3 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 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 [41]
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 [41]
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
WO2017089895A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.03 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 [41]
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 4 Reporting the Activity Date of This ADC [41]
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 [41]
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
WO2017089895A1 ADC44 [Investigative]
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 [41]
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 [41]
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 [41]
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
WO2017089895A1 ADC42 [Investigative]
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 [41]
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 [41]
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 [41]
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
WO2017089895A1 ADC38 [Investigative]
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 [41]
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 [41]
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 [41]
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
WO2017089895A1 ADC6 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 [41]
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 [41]
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 [41]
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 5 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC6 [Investigative]
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 [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC38 [Investigative]
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 [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
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
WO2017089890A1 ADC42 [Investigative]
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 [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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 [28]
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
WO2017089890A1 ADC44 [Investigative]
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 [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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 [28]
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
WO2017089890A1 ADC48 [Investigative]
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 [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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 [28]
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
WO2017089890A1 ADC50 [Investigative]
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 [28]
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 [28]
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 [28]
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
WO2017089895A1 ADC55 [Investigative]
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 [41]
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 [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC46 [Investigative]
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 [28]
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 [28]
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 [28]
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
WO2007011968A2 cAC10-9b [Investigative]
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 [37]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 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 [37]
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 Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 3 Reporting the Activity Date of This ADC [37]
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
WO2017089895A1 ADC69 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 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 [41]
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 3 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.14 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 4 Reporting the Activity Date of This ADC [41]
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
WO2017089895A1 ADC54 [Investigative]
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 [41]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC16 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 2 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.07 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 [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
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
Anti-HER2 DVD-IgG1_MMAF [Investigative]
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 [44]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [44]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10.00 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Anti-HER2 DVD-IgG1-h38c2-K99C_MMAF [Investigative]
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 [44]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.05 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [44]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10.00 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

   Click to Show/Hide
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
WO2017089890A1 ADC54 [Investigative]
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 [28]
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 [28]
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 [28]
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
WO2017089895A1 ADC14 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 2 Reporting the Activity Date of This ADC [41]
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 3 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC16 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.06 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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
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
WO2017089895A1 ADC20 [Investigative]
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 [41]
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 [41]
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 ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC20 [Investigative]
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 [28]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.29 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 [28]
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
WO2017089890A1 ADC62 [Investigative]
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 [28]
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 2 Reporting the Activity Date of This ADC [28]
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
WO2017089895A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 [41]
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 3 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.15 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.42 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.

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In Vitro Model Esophageal adenocarcinoma OE19 cells CVCL_1622
Experiment 6 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.75 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.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.19 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.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.37 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 Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC [41]
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 were counted using SRB assay.

   Click to Show/Hide
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC14 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.09 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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.31 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 [28]
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
WO2017089890A1 ADC69 [Investigative]
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 [28]
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 [28]
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
WO2017089895A1 ADC18 [Investigative]
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 [41]
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 [41]
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 Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [41]
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
WO2017089895A1 ADC8 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 [41]
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 3 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.18 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 [41]
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 Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC [41]
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
WO2017089895A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [41]
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 [41]
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 Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [41]
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 Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.21 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 5 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC8 [Investigative]
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 [28]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 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 [28]
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
WO2017089890A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [28]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.32 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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.97 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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.21 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 [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC18 [Investigative]
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 [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC66 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 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 [41]
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
WO2017089890A1 ADC66 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.11 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 [28]
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
WO2017089890A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.42 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 werecounted using SRB assay.

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In Vitro Model Esophageal adenocarcinoma OE19 cells CVCL_1622
Experiment 4 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.75 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.

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In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.19 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.

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In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
ADC14-0810 [Investigative]
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 [45]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.25 nM
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. The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model Lung adenocarcinoma HCC827 cells CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC [45]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
6.54 nM
High EGFR expression (CD19 +++)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [45]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Low EGFR expression (EGFR +)
Method Description
Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells. The cells were incubated for 72 hours.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089895A1 ADC76 [Investigative]
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 [41]
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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [41]
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 were counted using SRB assay.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
WO2017089890A1 ADC76 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.27 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.

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In Vitro Model Breast ductal carcinoma JIMT-1 cells CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC [28]
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.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Anti-HER2 DVD-Fab_MMAF [Investigative]
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 [44]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.33 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [44]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10.00 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Anti-HER2 DVD-Fab-h38c2-K99C_MMAF [Investigative]
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 [44]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.33 nM
High HER2 expression (HER2+++)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

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In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [44]
Efficacy Data Half Maximal Effective Concentration (EC50) > 10.00 uM Negative HER2 expression (HER2-)
Method Description
Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO2 for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells.

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In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
WO2017089895A1 ADC64 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.47 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.30 nM
High 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 Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [41]
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
WO2017089890A1 ADC64 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.47 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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.30 nM
High 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 Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC [28]
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
FOLR1-Mal-Caproyl-Val-Cit-PABC-MMAF [Investigative]
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 [46]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.00 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 [46]
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 [46]
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 [46]
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
WO2017089895A1 ADC72 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.78 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.00 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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
3.85 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 [41]
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
WO2017089890A1 ADC72 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.78 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 [28]
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
WO2021044208A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [47]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.07 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 2 Reporting the Activity Date of This ADC [47]
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 Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [47]
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 [47]
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 Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC [47]
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
WO2017089895A1 ADC70 [Investigative]
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 [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.56 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 [41]
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
WO2017089890A1 ADC70 [Investigative]
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 [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.56 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 [28]
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
WO2021044208A1 ADC9 [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [47]
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 Mantle cell lymphoma JeKo-1 cells CVCL_1865
Experiment 2 Reporting the Activity Date of This ADC [47]
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 Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC [47]
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 [47]
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 Breast squamous cell carcinoma HCC1806 cells CVCL_1258
Experiment 5 Reporting the Activity Date of This ADC [47]
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
HER2-acetal-ADC 11 [Investigative]
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 [38]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
22.00 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 [38]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
100 nM
Negative 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 MDA-MB-231 cells CVCL_0062
WO2017089895A1 ADC67 [Investigative]
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 [41]
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 2 Reporting the Activity Date of This ADC [41]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 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
WO2017089890A1 ADC67 [Investigative]
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 [28]
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 2 Reporting the Activity Date of This ADC [28]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 33.30 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
1F6-Asn- (D)Lys-MMAF [Investigative]
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 [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
7.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Experiment 3 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
9.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
1F6-Met- (D)Lys-MMAF [Investigative]
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 [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
8.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Clear cell renal cell carcinoma Caki-1 cells CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
10.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Renal cell carcinoma 786-O cells CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC [36]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
123.00 ng/mL
Positive TNF expression (TNF+++/++)
Method Description
IC50 values are the mean and SD of 21 independent experimental titrations, each performed at least in duplicate.
In Vitro Model Hodgkin lymphoma L-428 cells CVCL_1361
Anti-CD19(LC)-G7VIM-2i [Investigative]
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 [34]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
110 ng/mL
Positive CD19 expression (CD19 +++/++)
Method Description
Raji cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model EBV-related Burkitt lymphoma Raji cells CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC [34]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 10.00 ug/mL Negative CD19 expression (CD19 -)
Method Description
K562 cells were seeded in a 96-wellplate at 200,000 cells/well in 100 pL of growth media. The cells were incubated at 37°Cin 5% CO2, for 1 day. Serial dilutions of anti-CD19 ADC from 4.0 ug/mL to 1.5625 ng/mL in 100 pL media were added tothe wells, and the cells were incubated with the antibodies for 72 hours.
In Vitro Model Chronic myeloid leukemia K562 cells CVCL_0004
DAR4-ARC-ADC [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [48]
Efficacy Data Half Maximal Effective Concentration (EC50)
25.00 pM
Positive CLL-1 expression (CLL-1+++/++)
Method Description
In vitro cytotoxicity of the anti-hCLL-1 ARC-ADCs was then evaluated using human AML cell lines U937 (CLL-1+) and KG1a (CLL-1-1).
In Vitro Model Adult acute monocytic leukemia U-937 cells CVCL_0007
DAR2-ARC-ADC [Investigative]
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [48]
Efficacy Data Half Maximal Effective Concentration (EC50)
0.90 nM
Positive CLL-1 expression (CLL-1+++/++)
Method Description
In vitro cytotoxicity of the anti-hCLL-1 ARC-ADCs was then evaluated using human AML cell lines U937 (CLL-1+) and KG1a (CLL-1-1).
In Vitro Model Adult acute monocytic leukemia U-937 cells CVCL_0007
AGS-16C3F [Terminated in phase 2]
Identified from the Human Clinical Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [49]
Efficacy Data Partial Response (PR)
23.08%
High ENPP3 expression (ENPP3+++)
Patients Enrolled
Metastatic renal cell carcinoma (MRCC), Eastern Cooperative Oncology Group (ECOG) performance status 1, adequate organ and bone marrow function.
Administration Dosage
AGS-16M8F was administered intravenously every 3 weeks at 5 dose levels ranging from 0.60 to 4.80 mg/kg until unacceptable toxicity or progression. A second study with AGS-16C3F started with the AGS-16M8F bridging dose of 4.80 mg/kg given every 3 weeks.
Related Clinical Trial
NCT Number NCT01672775  Phase Status Phase 1
Clinical Description
A phase 1, open label, multi-center study to assess the safety, pharmacokinetics and effectiveness of AGS-16C3F monotherapy in subjects with renal cell carcinoma (RCC) of clear cell or papillary histology.
Primary Endpoint
In the AGS-16C3F study (n = 34),the MTD was 3.60 mg/kg,but this was not tolerated. The 1.80 mg/kg dose was determined to be safe and was associated antitumor response.
Other Endpoint
3 subjects at 1.80 mg/kg achieved durable PR (3/13, 23.08%). The disease control rate at 1.80 mg/kg was 92.30% (N=12/13). The disease control rate for the entire study was 58.82% (N=20/34).
Experiment 2 Reporting the Activity Date of This ADC [50]
Efficacy Data Objective Response Rate (ORR)
7.50% (AGS16C3F)
18.20% (axitinib)
Moderate ENPP3 expression (ENPP3++)
Patients Enrolled
Advanced renal cell carcinoma (RCC).
Administration Dosage
Intravenous AGS-16C3F 1.80 mg/kg every 3 weeks or oral axitinib 5 mg twice daily (starting dose).
Related Clinical Trial
NCT Number NCT02639182  Phase Status Phase 2
Clinical Description
A multi-center, open label, randomized phase 2 study of AGS-16C3F vs. axitinib in metastatic renal cell carcinoma.
Primary Endpoint
Median PFS=2.90 months (95% CI,2.00-4.00) for AGS16C3F,Median PFS=5.7 months (95% CI,5.30-9.10) for axitinib.
Other Endpoint
Disease Control Rate (DCR)=13.40% (95% CI,6.3-24.0) for AGS16C3F, Disease Control Rate (DCR)=22.70% (95% CI,13.30-34.70) for axitinib. Median duration of Response (mDoR)=6.80 months (95% CI,3.80-18.40) for AGS16C3F, Median duration of Response (mDoR)=6.7 months (95% CI,1.80-9.20) for axitinib. Objective Response Rate (ORR)=7.50% (95% CI,2.50-16.60) for AGS16C3F, Objective Response Rate (ORR)=18.20% (95% CI,9.80-29.60) for axitinib. Median Overall Survival (mOS)=13.10 months for AGS16C3F, Median Overall Survival (mOS)=15.40 months for axitinib.

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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 [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.10 nM
Method Description
Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model Normal ROSA KIT D816V cells CVCL_5G50
Experiment 2 Reporting the Activity Date of This ADC [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
2.73 nM
Moderate ENPP3 expression (ENPP3++)
Method Description
Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model Mast-cell sarcoma ROSA KIT D816V Gluc cells Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
109.90 nM
High ENPP3 expression (ENPP3+++)
Method Description
Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model Mast cell leukemia HMC-1.1 cells CVCL_H206
Experiment 4 Reporting the Activity Date of This ADC [51]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
146.50 nM
Method Description
Cells were incubated in triplicate in medium containing AGS-16C3F or cHmLYS-1c3.G2k-mcMMAF (0 [Control],0.001,0.003,0.008,0.02,0.07,0.21,0.62,1.82,5.57,16.67,50,150,450,and 1350 nM) in a 5% CO2 incubator at 37°C for 96 hours. IC50 values at day 5 for AGS-16C3F were calculated for each cell line.
In Vitro Model Mast cell leukemia HMC-1.2 cells CVCL_H205
MEDI-547 [Terminated in phase 1]
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 [52]
Efficacy Data Objective Response Rate (ORR)
0.00%
Patients Enrolled
Malignant solid tumor thought to be associated with increased expression of EphA2 (endometrial, breast, ovarian, prostate, non-small cell lung, colon, esophageal, gastric, and bladder cancers, renal cell carcinoma, melanoma), relapsed or refractory to standard therapy, and an Eastern Cooperative Oncology Group (ECOG) performance status score of 0-2.

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Administration Dosage
0.08 mg/kg, 1-h intravenous (IV) infusion once q3wks or qwk for 3 consecutive weeks until unacceptable toxicity, progressive disease.
Related Clinical Trial
NCT Number NCT00796055  Phase Status Phase 1
Clinical Description
A phase 1, open-label study of MEDI-547 to evaluate the safety, tolerability, pharmacokinetics, and biologic activity of intravenous administration in subjects with relapsed or refractory solid tumors associated with epha2 expression.
Primary Endpoint
Best response included progressive disease (n=5, 83.33%) and stable disease (n=1, 16.67%), No complete or partial tumor responses.
Other Endpoint
MTD could not be selected.
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [53]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 48.00% Negative EPHA2 expression (EPHA2-)
Method Description
Mice injected with EphA2-negative SPEC-2 cell was assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
In Vivo Model Endometrial cancer CDX model
In Vitro Model Endometrial cancer Endometrial cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [53]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.67% Positive EPHA2 expression (EPHA2+++/++)
Method Description
Mice injected with either Hec-1A or Ishikawa were assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
In Vivo Model Endometrial cancer CDX model
In Vitro Model Endometrial adenocarcinoma HEC-1-A cells CVCL_0293
Experiment 3 Reporting the Activity Date of This ADC [53]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.00% Positive EPHA2 expression (EPHA2+++/++)
Method Description
Mice injected with either Hec-1A or Ishikawa were assigned to one of four groups (n = 10 mice per group),MEDI-547,3 mg/kg weekly.
In Vivo Model Endometrial cancer CDX model
In Vitro Model Endometrial adenocarcinoma Ishikawa cells CVCL_2529
PF-06263507 [Terminated in phase 1]
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 [54]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.70% (Day 60) Low 5T4 expression (5T4+)
Method Description
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of PF-06263507 was 3 mg/kg Q4D 4.

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In Vivo Model Lung cancer CDX model
In Vitro Model Lung cancer Lung cancer cells Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC [54]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% (Day 60) Low 5T4 expression (5T4+)
Method Description
ASN004 was evaluated for efficacy in human tumor mouse xenograft models,derived from four different human tumor cell types,having a wide range of 5T4 expression levels. ASN004 was further evaluated in a tumor xenograft model derived from the H1975 human lung carcinoma cell line [5T4+; 15, 800 binding sites per cell]. Subcutaneous tumor xenografts were developed in nude mice with established mean tumor volumes of 150 mm3. The dose of PF-06263507 was 10 mg/kg Q4D 4.

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In Vivo Model Lung cancer CDX model
In Vitro Model Lung cancer Lung cancer cells Homo sapiens
References
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Ref 11 Safety and unique pharmacokinetic profile of ARX788, a site-specific ADC, in heavily pretreated patients with HER2-overexpresing solid tumors: Results from two phase 1 clinical trials. J Clin Oncol. 2021 39:15_suppl, 1038-1038.
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Ref 14 A Randomized, Open Label, Multi-center Phase II-III Neoadjuvant Study Comparing the Efficacy and Safety of ARX788 Combined With Pyrotinib Maleate Versus TCBHP (Trastuzumab Plus Pertuzumab With Docetaxel and Carboplatin) in Patients With HER2-positive Breast Cancer, NCT05426486
Ref 15 A Global Phase 2 Study to Evaluate the Efficacy and Safety of ARX788 for Selected HER2-mutated or HER2-amplified/Overexpressed Solid Tumors, NCT05041972
Ref 16 A Prospective, Single-arm, Single-center Phase II Clinical Study of Recombinant Humanized Anti-HER2 Monoclonal Antibody-AS269 Conjugate (ARX788) in the Treatment of HER2-positive Breast Cancer Patients With Brain Metastases, NCT05018702
Ref 17 A Single-arm, Single-center Phase II Clinical Study of Recombinant Humanized Anti-HER2 Monoclonal Antibody-AS269 Conjugate (ARX788) in the Treatment of Unresectable and/or Metastatic Breast Cancer With Low Expression of HER2, NCT05018676
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Ref 19 I-SPY Trial (Investigation of Serial Studies to Predict Your Therapeutic Response With Imaging And moLecular Analysis 2), NCT01042379
Ref 20 A Phase 1, Multicenter, Open-label, Multiple Dose-escalation Study of ARX788, Intravenously Administered as a Single Agent in Subjects With Advanced Cancers With HER2 Expression, NCT02512237
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