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Defactinib hydrochloride inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner, which may prevent the integrin-mediated activation of several downstream signal transduction pathways. RPPA data shows that VS-6063 reduces levels of AKT and YB-1 in taxane-resistant cell lines.
In vivo, Defactinib hcl doses of 25 mg/kg twice a day or greater statistically significantly inhibits pFAK (Tyr397) at 3 hours, with return of expression noted by 24 hours.
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Preparation method | |
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Incubation time |
Animal Experiment | |
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Animal models | Mice |
Formulation | prepared in phosphate-buffered saline |
Dosages | 25 mg/kg twice every day |
Administration | orally |
Molecular Weight | 546.95 |
Formula | C20H22ClF3N8O3S |
CAS Number | 1073160-26-5 |
Solubility (25°C) | DMSO: ≥ 25 mg/mL (Need ultrasonic) |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Lee BY, et al. Pharmacol Ther. FAK signaling in human cancer as a target for therapeutics.
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