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Background Information:
GSK2256098 is an orally bioavailable small molecule inhibitor of Focal adhesion kinase (FAK) (Ezymatic apparent Ki = 0.4 nM) , targeting specifically at phosphorylation site of the enzyme, tyrosine (Y) 397 (FAK Y397). GSK2256098 inhibition of FAK Y397 phosphorylation correlated with decreased levels of phosphorylated Akt and ERK in L3.6P1 cells (Cellular IC50 = 2-15 nM) , decreased cell viability, anchorage-independent growth, and motility in a dose dependent manner. (ref. 1-3). It is currently in clinical evaluation for cancer treatment.
Reference:
1. Zhang J, et al. Cell Cycle. 2014, 13(19):3143-9.
2. Auger, K. R. et. Al, The Focal Adhesion Kinase Inhibitor GSK2256098: a Potent and Selective Inhibitor for the Treatment of Cancer. Eur J Cancer, 2012, 48: 118.
3. Thanapprapa.sr D, et al, PTEN Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in Uterine Cancer, Mol Cancer Ther. 2015 Jun; 14(6):1466-75.
APIM050165: GSK2256098
CAS No.: 1224887-10-8.
Molecular Formula: C20H23ClN6O2 • 1/2H2O.
Molecular Weight: 423.9.
Purity: >99.5% by HPLC.
QC: HPLC-MS, NMR and Quantitative Elemental Analysis.
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