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Background Information:
Focal adhesion kinase (FAK), a non-receptor tyrosine kinase , orchestrates cell signaling through integrins and growth factor receptors and plays important roles in tumorigenesis. Defactinib is a potent, selective, and orally active FAK inhibitor with demonstrated tolerability and preliminary clinical activity targeting cancer stem cells, working as a single agent as well as in combination with paclitaxel.
Reference:
1. C. M. Vidal, et al., Abstract C271: FAK inhibitor defactinib (VS-6063) enhances the efficacy of paclitaxel and preferentially targets ovarian cancer stem cells, Mol Cancer Ther November 2013 12; C271.
APIM050141: DEFACTINIB (VS-6063, PF-04554878)
CAS No.: 1073154-85-4.
Molecular Formula: C20H21F3N8O3S ? 0.8HCl.
Molecular Weight: 539.7.
Purity: >99% (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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