General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GYOEJ
ADC Name
GABRP Ab-DM1 ADC
Synonyms
GABRP-Ab DM1
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Triple negative breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
3.8
Antibody Name
GABRP-Ab
 Antibody Info 
Antigen Name
Gamma-aminobutyric acid receptor subunit pi (GABRP)
 Antigen Info 
Payload Name
Mertansine DM1
 Payload Info 
Therapeutic Target
Microtubule (MT)
 Target Info 
Linker Name
Succinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate (SMCC)
 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 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
100 - 500
ng/mL
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
100 - 500
ng/mL
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 500
ng/mL
HCC1143 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 500
ng/mL
MDA-MB-231 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 500
ng/mL
BT-474 cells
Invasive breast carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
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 Inhibitory Concentration (IC50) 100 ng/mL - 500 ng/mL Positive GABRP expression (GABRP+++/++)
Method Description
Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 100 ng/mL - 500 ng/mL Positive GABRP expression (GABRP+++/++)
Method Description
Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 ng/mL Positive GABRP expression (GABRP+++/++)
Method Description
Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model Breast ductal carcinoma HCC1143 cells CVCL_1245
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 ng/mL Positive GABRP expression (GABRP+++/++)
Method Description
Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 500 ng/mL Positive GABRP expression (GABRP+++/++)
Method Description
Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
References
Ref 1 Identification and Validation of a Novel Biologics Target in Triple Negative Breast Cancer. Sci Rep. 2019 Oct 17;9(1):14934. doi: 10.1038/s41598-019-51453-w.

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