Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0RJITI
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| ADC Name |
CNTO95-SSNPP-DM4
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| Synonyms |
CNTO95 SSNPP DM4
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| Organization |
Sanofi SA
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| Drug Status |
Investigative
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| Indication |
In total 3 Indication(s)
Colon cancer [ICD11:2B90]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Melanoma [ICD11:2C30]
Investigative
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| Drug-to-Antibody Ratio |
3-4
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| Antibody Name |
CNTO95
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Antibody Info | ||||
| Antigen Name |
Integrin alpha-V (ITGAV)
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Antigen Info | ||||
| Payload Name |
Mertansine DM4
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Sulfosuccinimidyl-N-succinimidyl-4-(5-nitro-2-pyridyldithio) pentanoate (SSNPP)
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Linker Info | ||||
| Conjugate Type |
Random conjugation through nucleophilic lysines.
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% (Day 37) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
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| In Vivo Model | HT-29 CDX model | ||||
| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 71.21% (Day 24) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (5 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
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| In Vivo Model | A375.S2 CDX model | ||||
| In Vitro Model | Amelanotic melanoma | A375.S2 cells | CVCL_0136 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 77.15% (Day 24) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (10 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
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| In Vivo Model | A375.S2 CDX model | ||||
| In Vitro Model | Amelanotic melanoma | A375.S2 cells | CVCL_0136 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 95.10% (Day 49) | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
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| In Vivo Model | A549 CDX model | ||||
| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 1.00 ug/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 1.00 ug/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 1.20 ug/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 1.50 ug/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.19 mg/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.27 mg/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.27 mg/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | A2780 cells | CVCL_0134 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.29 mg/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Colon cancer | HT29 cells | CVCL_A8EZ | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.30 mg/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Ovarian endometrioid adenocarcinoma | A2780 cells | CVCL_0134 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) | 0.42 mg/mL | Positive ITGAV expression (ITGAV +++/++) | ||
| Method Description |
Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
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| In Vitro Model | Lung adenocarcinoma | A-549 cells | CVCL_0023 | ||
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