The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel.
|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 5 mg/mL;Water <1 mg/mL|
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). PMID: 24062525.
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Defactinib hydrochloride is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.
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.
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