Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0ZXCSM
ADC Name
Trastuzumab-RSL3-NH2
Organization
University of Grenoble Alpes
Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
7.9
Structure
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
RSL3-NH2
  Payload Info 
Therapeutic Target
Phospholipid hydroperoxide glutathione peroxidase (GPX4)
  Target Info 
Linker Name
Mal-PEG4-DBCO-Ala-Val
  Linker Info 
Conjugate Type
The free thiols in the reduced mAb was conjugated to the maleimide moiety of the dibenzocyclooctyne-PEG4-maleimide.
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) 
100
nM
BT-474 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 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 100.00 nM High HER2 expression (HER2+++)
Method Description
The inhibitory activity of Trastuzumab-RSL3-NH2 against cancer cell growth was evaluated by MTT cytotoxicity assay.
In Vitro Model Invasive breast carcinoma BT-474 cells CVCL_0179
References
Ref 1 The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead. Eur J Med Chem. 2022 Dec 15;244:114863.

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