Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ELKKR
ADC Name
Trastuzumab biosimilar mil40 12b
Synonyms
Trastuzumab-biosimilar-mil40-12b
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Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
4
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 Val-Ala-PABC linker 12b
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
General Information of The Activity Data Related to This ADC
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) 
0.03
nM
SK-BR-3 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.05
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.1
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.21
nM
SK-OV-3 cells
Ovarian serous cystadenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
11.51
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
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) 0.03 nM Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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) 0.05 nM Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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) 0.10 nM Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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) 0.21 nM Positive HER2 expression (HER2 +++/++)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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) 11.51 nM Negative HER2 expression (HER2 -)
Method Description
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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
Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
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. doi: 10.1080/10717544.2022.2039807.

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