Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GPRRL
ADC Name
EP3838893B1-ADC-C
Synonyms
MAB-W'-C6-PEG8'-Val-Ala-PAB-MMAE
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Organization
Academy of Military Medical Sciences
Drug Status
Investigative
Drug-to-Antibody Ratio
4;8
Structure
Antibody Name
mil40
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Monomethyl auristatin E
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
Mm-C6-PEG8'-Val-Ala-PAB
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
Mm-C6-PEG8'-Val-Ala-PAB-MMAE
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) 
0.064
nM
CVCL_0179
Invasive breast carcinoma
Half Maximal inhibitory Concentration (lC50) 
30.219
nM
CVCL_0031
Invasive breast carcinoma
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) 0.064 nM Positive HER2 expression (HER2+++/++)
Method Description
BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.

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In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) 30.219 nM Negative HER2 expression (HER2-)
Method Description
MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.

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In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Linker, antibody-drug conjugate including same, and uses thereof