General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0EPIMA
ADC Name
Neolymphostin ADC 21
Synonyms
Neolymphostin-ADC-21
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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
1.6
Antibody Name
Trastuzumab A114C
 Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
 Antigen Info 
Payload Name
Neolymphostin A
 Payload Info 
Therapeutic Target
3-Phosphoinositide-dependent protein kinase 1 (PDPK1)
 Target Info 
Linker Name
Mc-Val-Cit-PABC-DMEA
 Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines (A114C).
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
77.3
nM
BT-474 cells
Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50) 
225
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 1000
nM
MDA-MB-361 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 1000
nM
MDA-MB-468 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 77.30 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 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 225 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 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000 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-361 cells CVCL_0620
Experiment 4 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-468 cells CVCL_0419
References
Ref 1 Novel PIKK inhibitor antibody-drug conjugates: Synthesis and anti-tumor activity. Bioorg Med Chem Lett. 2019 Apr 1;29(7):943-947. doi: 10.1016/j.bmcl.2019.01.009. Epub 2019 Jan 11.

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