Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0FRNON
ADC Name
Cys-linker-MMAE-based ADC 15
Synonyms
Cys-15 MMAE
   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
3.88
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
Mc-PABC
  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 2 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 69.34
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 92.21
%
NCI-N87 cells
Gastric tubular adenocarcinoma
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) 
0.09
nM
HCC1954 cells
Breast ductal carcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.12
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.35
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
97.62
nM
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
110.54
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 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.34% (Day 60) High HER2 expression (HER2 +++)
Method Description
An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (5 mg/kg) on days 0, 7, 14, and 21.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.21% (Day 60) High HER2 expression (HER2 +++)
Method Description
An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (10 mg/kg) on days 0, 7, 14, and 21.
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 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.09 nM High HER2 expression (HER2 +++)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Breast ductal carcinoma HCC1954 cells CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.12 nM High HER2 expression (HER2 +++)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
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) 0.35 nM High HER2 expression (HER2 +++)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
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) 97.62 nM Negative HER2 expression (HER2-)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 110.54 nM Negative HER2 expression (HER2-)
Method Description
Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model Invasive breast carcinoma MCF-7 cells CVCL_0031
References
Ref 1 Antibody-Drug Conjugate Using Ionized Cys-Linker-MMAE as the Potent Payload Shows Optimal Therapeutic Safety. Cancers (Basel). 2020 Mar 21;12(3):744. doi: 10.3390/cancers12030744.

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