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.
|Formulation||prepared in phosphate-buffered saline|
|Dosages||25 mg/kg twice every day|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 25 mg/mL (Need ultrasonic)|
FAK signaling in human cancer as a target for therapeutics.
Lee BY, et al. Pharmacol Ther. 2015 Feb;146:132-49. PMID: 25316657.
Role of focal adhesion kinase in regulating YB-1-mediated paclitaxel resistance in ovarian cancer.
Kang Y, et al. J Natl Cancer Inst. 2013 Oct 2;105(19):1485-95. PMID: 24062525.
|Related FAK Products|
GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM.
Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.
PF-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM.
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor.
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