Payload Information
General Information of This Payload
Payload ID | PAY0QLDVX |
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Name | Monomethyl auristatin F |
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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 |
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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 |
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PubChem CID | ||||||
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
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InChIKey |
MFRNYXJJRJQHNW-DEMKXPNLSA-N
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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
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Pharmaceutical Properties | Molecule Weight |
732 |
Polar area |
167 |
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Complexity |
1160 |
xlogp Value |
2.1 |
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Heavy Count |
52 |
Rot Bonds |
21 |
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Hbond acc |
9 |
Hbond Donor |
4 |
The activity data of This Payload
Standard Type | Value | Units | Cell line | Disease Model | Cell line ID | Reference |
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Half Maximal Inhibitory Concentration (IC50) | 10 | nM |
HT-29 cells
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Colon adenocarcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 105 | nM |
H3396 cells
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Breast carcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 137 | nM |
HL-60 cells
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Adult acute myeloid leukemia
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 2880 | nM |
HCT 116 cells
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Colon carcinoma
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[1] | |
Half Maximal Inhibitory Concentration (IC50) | 5.3 | nM |
SK-BR-3 cells
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Breast adenocarcinoma
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[2] | |
Half Maximal Inhibitory Concentration (IC50) | 7 | nM |
Hep-G2 cells
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Hepatoblastoma
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[3] | |
Half Maximal Inhibitory Concentration (IC50) | 8.8 | nM |
BT474-M1 cells
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Invasive breast carcinoma
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[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
Experiment 1 Reporting the Activity Date of This ADC | [4] | ||||
Efficacy Data | Objective Response Rate (ORR) |
60.00%
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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.
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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.
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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%).
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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%
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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.
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Administration Dosage |
GSK2857916 3.4 mg/kg was administered through 1-h intravenous infusions once every 3 weeks, for a maximum of 16 cycles.
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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.
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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.
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Other Endpoint |
The median progression-free survival was 12.00 months and the median duration of response was 14.30 months.
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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
Experiment 1 Reporting the Activity Date of This ADC | [7] | ||||
Efficacy Data | Half Maximal Effective Concentration (EC50) |
30.60 ug/mL
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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).
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In Vitro Model | Thymoma | EL4 cells (BCMA expression) | CVCL_0255 |
ARX-788 [Phase 3]
Identified from the Human Clinical Data
Experiment 1 Reporting the Activity Date of This ADC | [8] | ||||
Efficacy Data | Objective Response Rate (ORR) |
57.10%
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Patients Enrolled |
Patients with HER2+ mBC whose disease has progressed following T-DM1, T-DXd, and/or tucatinib-containing regimens.
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Administration Dosage |
Administered with an initial dose of 1.50 mg/kg Q4W and subsequent doses of 1.30 mg/kg Q4W.
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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.
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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) |
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Patients Enrolled |
Twenty-two (73.30%) had gastric adenocarcinoma, and the rest (26.70%) had GEJ adenocarcinoma.
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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.
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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%
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Patients Enrolled |
HER2-positive advanced gastric/gastroesophageal junction adenocarcinoma failing to respond to prior trastuzumab-based standard treatment, at least one dose.
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Administration Dosage |
9 patients received 1.30 mg/kg, 14 received 1.50 mg/kg, and 7 received 1.70 mg/kg ARX788.
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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.
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Experiment 4 Reporting the Activity Date of This ADC | [10] | ||||
Efficacy Data | Objective Response Rate (ORR) |
65.52%
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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.
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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].
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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).
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Experiment 5 Reporting the Activity Date of This ADC | [11] | ||||
Efficacy Data | Objective Response Rate (ORR) |
74.00% (Breast cancer)
67.00% (Pan-tumor) |
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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).
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Administration Dosage |
0.33 - 1.5 mg/kg; Q3W or Q4W.
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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.
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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.
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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.
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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.
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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.
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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.
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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).
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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.
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LCB14-0110 [Phase 3]
Identified from the Human Clinical Data
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) |
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Patients Enrolled |
Patients with HER2-expresssing advanced solid tumors who had failed prior standard of care therapies.
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Administration Dosage |
FS-1502 was given IV once in 21-day or 28-day cycle at doses of 0.10-3.50 mg/kg.
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Depatuxizumab mafodotin [Phase 3]
Identified from the Human Clinical Data
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)
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High EGFR expression (EGFR +++) | ||
Patients Enrolled |
EGFR-amp newly diagnosed GBM were randomized 1:1 to radiotherapy, temozolomide, and depatux-m/placebo.
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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.
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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)
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High EGFR expression (EGFR +++) | ||
Patients Enrolled |
EGFR-amp newly diagnosed GBM were randomized 1:1 to radiotherapy, temozolomide, and depatux-m/placebo.
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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.
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Revealed Based on the Cell Line Data
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.
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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
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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.
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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
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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.
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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
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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.
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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
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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.
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In Vitro Model | Pleural mesothelioma | NCI-H2052 cells | CVCL_1518 |
GPC-1-ADC [Investigative]
Discovered Using Patient-derived Xenograft Model
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.
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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.
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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.
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In Vivo Model | Pancreatic cancer PDX model |
Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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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.
|
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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
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.
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||||
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
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.
|
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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.
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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.
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||||
In Vivo Model | Bladder cancer PDX model (PDX: AG-B8) |
Discovered Using Cell Line-derived Xenograft Model
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.
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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
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.
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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.
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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
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.
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In Vitro Model | Colon carcinoma | HCT 116 cells | CVCL_0291 |
GPC-1 ADC 1 [Investigative]
Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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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.
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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.
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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.
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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
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
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.
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||||
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.
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||||
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.
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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.
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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
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.
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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.
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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.
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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.
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In Vitro Model | Plasma cell myeloma | MM1.S cells | CVCL_8792 |
Ab3-mcMMAF [Investigative]
Discovered Using Cell Line-derived Xenograft Model
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.
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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
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.
|
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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
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
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).
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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).
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||||
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
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
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.
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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
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.
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||||
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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.
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) |
0.35 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
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
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
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
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
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
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
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
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).
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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).
|
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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
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.
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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 |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 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.
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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) |
0.09 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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|
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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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|
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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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|
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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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|
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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
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
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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|
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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
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.
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||||
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.
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||||
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.
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||||
In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 |
ZHER2-ABD-mcMMAF [Investigative]
Revealed Based on the Cell Line Data
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.
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||||
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.
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||||
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
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.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC62 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.08 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.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.05 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.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC40 [Investigative]
Revealed Based on the Cell Line Data
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
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.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC53 [Investigative]
Revealed Based on the Cell Line Data
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.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC50 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.05 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 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 ADC48 [Investigative]
Revealed Based on the Cell Line Data
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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|
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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.
|
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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) |
0.08 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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|
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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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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
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
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
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
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
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
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) |
0.38 nM
|
Moderate HER2 expression (HER2++) | ||
Method Description |
Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.
Click to Show/Hide
|
||||
In Vitro Model | Breast ductal carcinoma | JIMT-1 cells | CVCL_2077 | ||
Experiment 3 Reporting the Activity Date of This ADC | [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 ADC38 [Investigative]
Revealed Based on the Cell Line Data
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 |
WO2017089890A1 ADC42 [Investigative]
Revealed Based on the Cell Line Data
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) |
0.04 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
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 |
WO2017089890A1 ADC48 [Investigative]
Revealed Based on the Cell Line Data
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) |
0.08 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
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.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC55 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
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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) |
0.07 nM
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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 |
WO2017089890A1 ADC46 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.04 nM
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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
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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 |
WO2007011968A2 cAC10-9b [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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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.
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In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 |
WO2017089895A1 ADC69 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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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.
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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
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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.
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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
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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.
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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.
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In Vitro Model | Chronic myeloid leukemia | K562 cells | CVCL_0004 |
WO2017089895A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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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
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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
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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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.
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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) |
0.06 nM
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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) |
0.07 nM
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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.
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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) |
0.26 nM
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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 |
Anti-HER2 DVD-IgG1_MMAF [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [44] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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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-IgG1-h38c2-K99C_MMAF [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [44] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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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 |
WO2017089890A1 ADC54 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.05 nM
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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
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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 ADC14 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
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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.
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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) |
0.08 nM
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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.
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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) |
0.09 nM
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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
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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
Experiment 1 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.06 nM
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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
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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 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
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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) |
0.29 nM
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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 |
WO2017089890A1 ADC20 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
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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) |
0.29 nM
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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 ADC62 [Investigative]
Revealed Based on the Cell Line Data
Experiment 1 Reporting the Activity Date of This ADC | [28] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.08 nM
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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 |
WO2017089895A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.14 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.
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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) |
0.15 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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|
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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.
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|
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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.
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|
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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.
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|
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC14 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.31 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.
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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 ADC69 [Investigative]
Revealed Based on the Cell Line Data
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.
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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
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.
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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) |
0.34 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.
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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 ADC8 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.11 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.
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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 |
WO2017089895A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
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.
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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) |
0.32 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.
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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) |
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.
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|
||||
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.
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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 | [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 ADC8 [Investigative]
Revealed Based on the Cell Line Data
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.
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|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC4 [Investigative]
Revealed Based on the Cell Line Data
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.
Click to Show/Hide
|
||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC18 [Investigative]
Revealed Based on the Cell Line Data
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 |
WO2017089895A1 ADC66 [Investigative]
Revealed Based on the Cell Line Data
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
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
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.
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) |
0.16 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
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.
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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.
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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.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC76 [Investigative]
Revealed Based on the Cell Line Data
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
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
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
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
Experiment 1 Reporting the Activity Date of This ADC | [41] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.47 nM
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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.
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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
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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.
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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.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089890A1 ADC64 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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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.
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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
Experiment 1 Reporting the Activity Date of This ADC | [46] | ||||
Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.00 nM
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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.
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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.
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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.
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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.
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In Vitro Model | Osteosarcoma | SJSA-1 cells | CVCL_1697 |
WO2017089895A1 ADC72 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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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.
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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.
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In Vitro Model | Chronic myeloid leukemia | K562 cells | CVCL_0004 |
WO2017089890A1 ADC72 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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In Vitro Model | Chronic myeloid leukemia | K562 cells | CVCL_0004 |
WO2021044208A1 ADC2 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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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.
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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.
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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.
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||||
In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
WO2017089895A1 ADC70 [Investigative]
Revealed Based on the Cell Line Data
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.
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||||
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
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
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.
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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.
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In Vitro Model | Invasive breast carcinoma | MCF-7 cells | CVCL_0031 |
HER2-acetal-ADC 11 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 |
WO2017089895A1 ADC67 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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In Vitro Model | Burkitt lymphoma | Ramos cells | CVCL_0597 |
WO2017089890A1 ADC67 [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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In Vitro Model | Burkitt lymphoma | Ramos cells | CVCL_0597 |
1F6-Asn- (D)Lys-MMAF [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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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.
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In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 |
1F6-Met- (D)Lys-MMAF [Investigative]
Revealed Based on the Cell Line Data
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.
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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.
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||||
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
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.
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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.
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In Vitro Model | Chronic myeloid leukemia | K562 cells | CVCL_0004 |
DAR4-ARC-ADC [Investigative]
Revealed Based on the Cell Line Data
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).
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In Vitro Model | Adult acute monocytic leukemia | U-937 cells | CVCL_0007 |
DAR2-ARC-ADC [Investigative]
Revealed Based on the Cell Line Data
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).
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In Vitro Model | Adult acute monocytic leukemia | U-937 cells | CVCL_0007 |
AGS-16C3F [Terminated in phase 2]
Identified from the Human Clinical Data
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.
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||||
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.
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||||
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).
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||||
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.
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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.
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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
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.
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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.
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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.
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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.
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In Vitro Model | Mast cell leukemia | HMC-1.2 cells | CVCL_H205 |
MEDI-547 [Terminated in phase 1]
Identified from the Human Clinical Data
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.
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||||
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.
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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.
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Discovered Using Cell Line-derived Xenograft Model
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.
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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.
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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.
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||||
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
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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