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BI-3663 - CAS 2341740-84-7

Inquiry

BI-3663 (BI 3663) is a cereblon-based degrader (PROTAC) of Focal adhesion tyrosine kinase (PTK2/FAK) with a median DC50 of 30 nM to >80% across a panel of eleven HCC cell lines; degraded PTK2 potently (DC50 = 27 nM) with a maximally obtainable degradation at the chosen experimental conditions of 95% (Dmax) in human lung adenocarcinoma cell line A549 after 16 hours treatment.

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Molecular Formula

C44H42F3N7O12

Molecular Weight

917.84

BI-3663

- Specification
  - Purity
    
    ≥95%
    
    Solubility
    
    Soluble in DMSO
    
    Appearance
    
    Solid Powder
    
    Storage
    
    Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
    
    Shipping
    
    Room temperature in continental US; may vary elsewhere
    
    IUPAC Name
    
    N-[2-[2-[2-[3-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethyl]-3-methoxy-4-[[4-[(3-oxo-1,2-dihydroinden-4-yl)oxy]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide
    
    Synonyms
    
    N-(2-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3-oxopropoxy)ethoxy)ethoxy)ethyl)-3-methoxy-4-((4-((3-oxo-2,3-dihydro-1H-inden-4-yl)oxy)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide; BI 3663; BI3663; Benzamide, 4-[[4-[(2,3-dihydro-3-oxo-1H-inden-4-yl)oxy]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-N-[2-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethyl]-3-methoxy-; 4-[[4-[(2,3-Dihydro-3-oxo-1H-inden-4-yl)oxy]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-N-[2-[2-[2-[3-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethyl]-3-methoxybenzamide
- Properties
  - Density
    
    1.456±0.06 g/cm3
    
    InChI Key
    
    ADTXLFJKQHYGPM-UHFFFAOYSA-N
    
    InChI
    
    InChI=1S/C44H42F3N7O12/c1-62-33-22-25(8-10-28(33)51-43-49-23-27(44(45,46)47)40(53-43)66-32-7-2-4-24-9-12-31(55)36(24)32)38(58)48-15-17-64-19-21-65-20-18-63-16-14-35(57)50-29-6-3-5-26-37(29)42(61)54(41(26)60)30-11-13-34(56)52-39(30)59/h2-8,10,22-23,30H,9,11-21H2,1H3,(H,48,58)(H,50,57)(H,49,51,53)(H,52,56,59)
    
    Canonical SMILES
    
    COC1=C(C=CC(=C1)C(=O)NCCOCCOCCOCCC(=O)NC2=CC=CC3=C2C(=O)N(C3=O)C4CCC(=O)NC4=O)NC5=NC=C(C(=N5)OC6=CC=CC7=C6C(=O)CC7)C(F)(F)F
- Reference Reading
  - 1. Highly selective PTK2 proteolysis targeting chimeras to probe focal adhesion kinase scaffolding functions.
    
    Popow, J., Arnhof, H., Bader, G., Berger, H., Ciulli, A., Covini, D., Dank, C., Gmaschitz, T., Greb, P., Karolyi-Özguer, J. and Koegl, M., 2019. Journal of Medicinal Chemistry, 62(5), pp.2508-2520.
    
    Focal adhesion tyrosine kinase (PTK2) is often overexpressed in human hepatocellular carcinoma (HCC), and several reports have linked PTK2 depletion and/or pharmacological inhibition to reduced tumorigenicity. However, the clinical relevance of targeting PTK2 still remains to be proven. Here, we present two highly selective and functional PTK2 proteolysis-targeting chimeras utilizing von Hippel-Lindau and cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 (cereblon-based) degrades PTK2 with a median DC50 of 30 nM to >80% across a panel of 11 HCC cell lines. Despite effective PTK2 degradation, these compounds did not phenocopy the reported antiproliferative effects of PTK2 depletion in any of the cell lines tested. By disclosing these compounds, we hope to provide valuable tools for the study of PTK2 degradation across different biological systems.

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