Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0BZLMR
ADC Name
ADC Mil40-6
Synonyms
NAC-6
   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
5.5
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
Silyl ether-based linker
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 93.6
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Maximum inhibition efficiency (MIE) 
< 10
%
MDA-MB-231 cells
Breast adenocarcinoma
Maximum inhibition efficiency (MIE) 
47.8
%
MCF-7 cells
Invasive breast carcinoma
Maximum inhibition efficiency (MIE) 
50.5
%
BT-474 cells
Invasive breast carcinoma
Maximum inhibition efficiency (MIE) 
87.3
%
MDA-MB-453 cells
Breast adenocarcinoma
Maximum inhibition efficiency (MIE) 
93.54
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.03
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.1
nM
MDA-MB-453 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.17
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
7.74
nM
MCF-7 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 1000
nM
MDA-MB-231 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.60% (Day 32) High HER2 expression (HER2+++)
Method Description
The animals were given vehicle, mil40, and ADC on days 0, 7, 14, and 21, and 4 intravenous injections of ADC at doses of 5 mg/kg.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Revealed Based on the Cell Line Data
Click To Hide/Show 10 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) < 10.00% Negative HER2 expression (HER2-)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 47.80% Negative HER2 expression (HER2-)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 50.50% High HER2 expression (HER2+++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 87.30% Moderate HER2 expression (HER2++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Maximum inhibition efficiency (MIE) 93.54% High HER2 expression (HER2+++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.03 nM High HER2 expression (HER2+++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.10 nM Moderate HER2 expression (HER2++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-453 cells CVCL_0418
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.17 nM High HER2 expression (HER2+++)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 7.74 nM Negative HER2 expression (HER2-)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000 nM Negative HER2 expression (HER2-)
Method Description
HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Novel Silyl Ether-Based Acid-Cleavable Antibody-MMAE Conjugates with Appropriate Stability and Efficacy. Cancers (Basel). 2019 Jul 8;11(7):957. doi: 10.3390/cancers11070957.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.