Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0OWIBE
ADC Name
TTZ-3-MMAE
Synonyms
TTZ-3 MMAE
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
3-4
Antibody Name
Trastuzumab
  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
DSPh-PEG12-Val-Ala-PABC
  Linker Info 
Conjugate Type
Site-specific conjugation 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 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
27.2
pM
SK-BR-3 cells
Breast adenocarcinoma
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) 27.20 pM Positive HER2 expression (HER2+++/++)
Method Description
Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model Breast adenocarcinoma SK-BR-3 cells CVCL_0033
References
Ref 1 Impact of cathepsin B-sensitive triggers and hydrophilic linkers on in vitro efficacy of novel site-specific antibody-drug conjugates. Org Biomol Chem. 2018 Mar 14;16(11):1882-1889. doi: 10.1039/c7ob02780j.

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