Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0WJFCK
ADC Name
39424599 ADC-S32A
Synonyms
ADC-S32A
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Organization
Eisai Inc.
Drug Status
Investigative
Drug-to-Antibody Ratio
0.6
Structure
Antibody Name
Morab-003
  Antibody Info 
Antigen Name
Folate receptor alpha (FOLR1)
  Antigen Info 
Payload Name
Undisclosed
Therapeutic Target
Stimulator of interferon genes protein (STING1)
  Target Info 
Linker Name
Electron-deficient Disulfide-based cleavable linker 32
  Linker Info 
Conjugate Type
Random conjugation through nucleophilic lysines
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal inhibitory Concentration (lC50) 
0.37
nM
CVCL_1304
Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma
Half Maximal inhibitory Concentration (lC50) 
12.005
nM
CVCL_1304
Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 0.37 nM Positive FR expression (FR+++/++)
Method Description
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.

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In Vitro Model Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma IGROV1 cells CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 12.005 nM Negative FR expression (FR-)
Method Description
IGROV1 (FRalpha+) and A431 (FRalpha-) cells were sub-cultured and seeded at 10,000 cells/well in complete growth medium in 96 well tissue culture plates, incubated at 37°C, 5% CO2 overnight (16 hours). Test reagents were serial diluted 1:3 in 2 mL deep-well dilution plates, starting at 200 nM (10 dilutions total). Diluted samples (100 uL) were added to the cell plates (starting concentration of test samples at 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 5 days. Medium was then discarded. The plates were washed once with 200 uL DPBS, stained with 50 uL of 0.2% Crystal Violet solution at room temperature for 15 min, and then washed extensively with tap water. Plates were air-dried, and Crystal Violet was dissolved with 200 uL of 1% SDS solution. Plates were read at 570 nm. Data was analyzed using GraphPad Prism 6.

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In Vitro Model Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma IGROV1 cells CVCL_1304
References
Ref 1 A Novel Concept for Cleavable Linkers Applicable to Conjugation Chemistry - Design, Synthesis and Characterization