Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0AYEUI
ADC Name
40H3-CL2A-SN38
Synonyms
40H3 CL2A SN38
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Triple negative breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
7.24
Structure
Antibody Name
Anti-EGFR mAb 40H3
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
Active metabolite of irinotecan SN38
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  Target Info 
Linker Name
CL2A
  Linker Info 
Conjugate Type
The free sulfhydryl group obtained by the reduction of interchain cysteine is site-specific conjugated with maleimide, michael addition reaction.
Combination Type
Govitecan
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
19.71
nM
A431 cells
Skin squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
27.83
nM
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
98.81
nM
BT-20 cells
Invasive breast carcinoma of no special type
Half Maximal Inhibitory Concentration (IC50) 
> 100
nM
MDA-MB-231 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 19.71 nM High EGFR expression (EGFR+++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 27.83 nM High EGFR expression (EGFR+++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 98.81 nM Moderate EGFR expression (EGFR++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Invasive breast carcinoma of no special type BT-20 cells CVCL_0178
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100.00 nM Negative EGFR expression (EGFR-)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Antibody drug conjugates, targeting cancer-expressed EGFR, exhibit potent and specific antitumor activity. Biomed Pharmacother. 2023 Jan;157:114047.

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