Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0RWPSE
ADC Name
Anti-FucGM1-48 ADC
Synonyms
Anti-FucGM1 48 ADC
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
1.9
Antibody Name
Anti-FucGM1 mAb
  Antibody Info 
Antigen Name
Fucosylated monosialotetrahexosylganglioside (FucGM1)
  Antigen Info 
Payload Name
Tetrahydroisoquinoline-based PBD dimer 17
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
PEG8-Val-Cit-PABC
  Linker Info 
Conjugate Type
Bacterial transglutaminase (BTGase)-mediated site-specific conjugation (Q295).
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
1.9
nM
NCI-H187 cells
Lung small cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.90 nM Positive FucGM1 expression (FucGM1+++/++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
References
Ref 1 Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385.

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