GSK2256098

• CAT Number: I000864
• CAS Number: 1224887-10-8
• Molecular Formula: C₂₀H₂₃ClN₆O₂
• Molecular Weight: 414.89
• Purity: ≥95%
• Target: FAK[1]
• Solubility: DMSO: ≥ 30 mg/mL
• Storage: Store at -20°C
• IUPAC Name: 2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-N-methoxybenzamide
• 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
• SMILES: CC1=NN(C(=C1)NC2=NC=C(C(=C2)NC3=CC=CC=C3C(=O)NOC)Cl)C(C)C

GSK2256098 (Cat.No:I000864) is a small molecule inhibitor developed by GlaxoSmithKline (GSK). It targets the focal adhesion kinase (FAK) by binding to its phosphorylation site, tyrosine (Y) 397, inhibiting FAK activity. GSK2256098 has shown potential in inhibiting FAK and its downstream signaling pathways, reducing cell survival, migration, and inducing apoptosis in various cancer cell lines. In preclinical studies, it demonstrated efficacy in pancreatic ductal adenocarcinoma (PDAC) and glioblastoma (GBM) models.

Reference

1:A phase I, pharmacokinetic and pharmacodynamic study of GSK2256098, a focal adhesion kinase inhibitor, in patients with advanced solid tumors. Soria JC, Gan HK, Blagden SP, Plummer R, Arkenau HT, Ranson M, Evans TR, Zalcman G, Bahleda R, Hollebecque A, Lemech C, Dean E, Brown J, Gibson D, Peddareddigari V, Murray S, Nebot N, Mazumdar J, Swartz L, Auger KR, Fleming RA, Singh R, Millward M.Ann Oncol. 2016 Dec;27(12):2268-2274. doi: 10.1093/annonc/mdw427. Epub 2016 Oct 11. PMID: 27733373 2:A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells. Zhang J, He DH, Zajac-Kaye M, Hochwald SN.Cell Cycle. 2014;13(19):3143-9. doi: 10.4161/15384101.2014.949550. PMID: 25486573 Free PMC Article