Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0LAXWY
ADC Name
H32-DM1_3.8
Synonyms
H32-DM1 3.8
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
3.8
Antibody Name
Anti-HER2 mAb H32
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  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.
Combination Type
Emtansine
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
0.05
nM
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.54
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.76
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.05 nM±0.05 nM High HER2 expression (HER2 +++)
Method Description
To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.54 nM±0.07 nM High HER2 expression (HER2 +++)
Method Description
To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.76 nM±0.15 nM High HER2 expression (HER2 +++)
Method Description
To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Preparation and characterization of antibody-drug conjugates acting on HER2-positive cancer cells. PLoS One. 2020 Sep 28;15(9):e0239813. doi: 10.1371/journal.pone.0239813. eCollection 2020.

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