NVP-TAE226, a potent dual FAK/IGF-1R, inhibiting FAK and IGF-1R with IC50 of 5.5 nM and 0.14 μM, respectively.
|Source||J Biol Chem (2011). Figure 8. NVP-TAE226|
|Cell Lines||HEK293 cells|
|Incubation Time||90 min|
|Results||To test the biological importance of the reciprocal RET-FAK transactivation, established HEK293 cells expressing a constitutively active RET mutant (RET C634R) were treated with the FAK kinase inhibitor NVP-TAE226|
|Cell lines||U87, U87 EGFR, U87 vIII and U251 cells|
|Preparation method||Cell Viability Assay
Cell cultures were harvested with 0.05% trypsin and seeded in triplicate at 2 × 104 in 24-well culture plates for 24 h before drug treatment. Culture medium was used for mock treatment. Cells were harvested at the indicated day after treatment, and viable cells were counted using the Vi-cell viability analyzer.
|Concentrations||1 and 10 μmol/L|
|Incubation time||1, 3 and 5 days|
|Animal models||U87 and LN229 glioma xenograft Intracranial Animal Model|
|Dosages||50 or 75 mg/kg once a day for 5 days and off for 2 days, for a duration of 4 weeks|
|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 70 mg/mL|
Inhibition of both focal adhesion kinase and insulin-like growth factor-I receptor kinase suppresses glioma proliferation in vitro and in vivo.
Liu TJ, et al. Mol Cancer Ther. 2007 Apr;6(4):1357-67. PMID: 17431114.
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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.
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