General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0DJNVI
ADC Name
CNTO95-SSNPB-DM4
Synonyms
CNTO95 SSNPB DM4
   Click to Show/Hide
Organization
Sanofi SA
Drug Status
Investigative
Indication
In total 3 Indication(s)
Colon cancer [ICD11:2B90]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Melanoma [ICD11:2C30]
Investigative
Drug-to-Antibody Ratio
3-4
Antibody Name
CNTO95
 Antibody Info 
Antigen Name
Integrin alpha-V (ITGAV)
 Antigen Info 
Payload Name
Mertansine DM4
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
N-sulfosuccinimidyl-4-(5-nitro-2 pyridyldithio) butyrate (SSNPB)
 Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 82.51
%
HT29 cells
Colon cancer
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Effective Concentration (EC50) 
0.24
ug/mL
HT29 cells
Colon cancer
Half Maximal Effective Concentration (EC50) 
0.3
ug/mL
A-549 cells
Lung adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.21
mg/mL
HT29 cells
Colon cancer
Half Maximal Effective Concentration (EC50) 
0.27
mg/mL
A2780 cells
Ovarian endometrioid adenocarcinoma
Half Maximal Effective Concentration (EC50) 
0.34
mg/mL
A-549 cells
Lung adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.51% (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).
In Vivo Model HT-29 CDX model
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Revealed Based on the Cell Line Data
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.24 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.
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) 0.30 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.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.21 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).
In Vitro Model Colon cancer HT29 cells CVCL_A8EZ
Experiment 4 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).
In Vitro Model Ovarian endometrioid adenocarcinoma A2780 cells CVCL_0134
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Effective Concentration (EC50) 0.34 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).
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
References
Ref 1 Anti-integrin immunoconjugates, methods and uses; 2008-01-17.

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