General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0VVVWC
ADC Name
Mil40-12B
Synonyms
Mil40 12b
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 4 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Breast ductal carcinoma [ICD11:2C61]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Drug-to-Antibody Ratio
4
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
Maleamic methyl ester-based linker 12B
 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) 
≈ 80
%
Breast ductal carcinoma cells
Breast ductal carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
25.8
pM
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
53.6
pM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
102.6
pM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
207.4
pM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
11.52
nM
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
26.44
nM
MCF-7 cells
Invasive breast carcinoma
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) ≈ 80.00% (Day 60) High HER2 expression (HER2+++)
Method Description
Mil40-12b induces efficient tumor cell killing in cell PDX models from a breast cancer patient with HER2 expression.
In Vivo Model Breast ductal carcinoma CDX model
In Vitro Model Breast ductal carcinoma Breast ductal carcinoma cells Homo sapiens
Revealed Based on the Cell Line Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 25.80 pM High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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) 53.60 pM High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 102.60 pM High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 207.40 pM High HER2 expression (HER2+++)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model Ovarian serous cystadenocarcinoma SK-OV-3 cells CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 11.52 nM Negative HER2 expression (HER2-)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 26.44 nM Negative HER2 expression (HER2-)
Method Description
To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Development of applicable thiol-linked antibody-drug conjugates with improved stability and therapeutic index. Drug Deliv. 2022 Dec;29(1):754-766.

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