GSK2256098
- GTPL7939
Axon 3717
CAS:
1224887-10-8
Purity:
99%
- Soluble in DMSO
- MF: C20H23ClN6O2
- MW: 414.89
Description
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.
More Information
| Parent CAS No. | 1224887-10-8 |
|---|---|
| Chemical Name | 2-(5-chloro-2-(1-isopropyl-3-methyl-1H-pyrazol-5-ylamino)pyridin-4-ylamino)-N-methoxybenzamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C=C(C(NOC)=O)C(NC2C(Cl)=CN=C(NC3=CC(C)=NN3C(C)C)C=2)=CC=1 |
| MFCD | MFCD30502650 |
| InChi | InChI=1S/C20H23ClN6O2/c1-12(2)27-19(9-13(3)25-27)24-18-10-17(15(21)11-22-18)23-16-8-6-5-7-14(16)20(28)26-29-4/h5-12H,1-4H3,(H,26,28)(H2,22,23,24) |
| InChiKey | BVAHPPKGOOJSPU-UHFFFAOYSA-N |
| CID | 46214930 |
| Short Description | FAK inhibitor |
References
- J. Zhang et al A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells. Cell Cycle. 2014,13, 3143-3149.
- N.F. Brown et. al The Focal Adhesion Kinase Inhibitor GSK2256098: a Potent and Selective Inhibitor for the Treatment of Cancer. Eur. J. Cancer, 2012, 48, 118.
- D. Thanapprapa et al, PTEN Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in Uterine Cancer, Mol Cancer Ther. 2015,14, 1466-1475.
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