Name: Defactinib
Price: 220.00 USD

- Overview
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    Background
    
    Defactinib is a selective, and orally active focal adhesion kinase (FAK) inhibitor [1].
    FAK is a nonreceptor tyrosine kinase involved in many oncogenic pathways. Increased expression of FAK has been observed in a number of tumor types, including breast, colon, and ovarian cancers. It has been reported that FAK inhibition can sensitize cancer cells to chemotherapy [1].
    In Taxane-sensitive (HeyA8) and Taxane-resistant (HeyA8-MDR) cell lines, Defactinib at 0 ~ 10 μM significantly inhibited pFAK (Tyr397) expression in a dose-dependent manner. In addition, simultaneous exposure to doses of Paclitaxel and Defactinib at ratios of 1:1000 for HeyA8 and 1:10 for HeyA8-MDR showed a synergistic inhibitory effect on cell growth [1].
    In mice bearing HeyA8 tumors, there was a 97.9% reduction in tumor weight by the combination therapy (Defactinib: 25 mg/kg orally twice daily, Paclitaxel: 2.5 mg/kg intraperitoneally weekly), compared with an 87.4% reduction in tumor weight by Paclitaxel monotherapy. In the SKOV3ip1 model, a 92.7% tumor weight reduction was observed in the combination group (Defactinib: 25 mg/kg orally twice daily, Paclitaxel: 2 mg/kg intraperitoneally weekly) [1].
- Properties
  - Alternative Name
    
    N-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide
    
    CAS Number
    
    1073154-85-4
    
    Molecular Formula
    
    C20H21F3N8O3S
    
    Molecular Weight
    
    510.49
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥160.2 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758

Defactinib

Defactinib

Background

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