GTPL7939 , 99% , 1224887-10-8

CAS NO.：1224887-10-8

Empirical Formula: C20H23ClN6O2

Molecular Weight: 414.89

MDL number:

PRODUCT Properties

• Density: 1.32±0.1 g/cm3(Predicted)
• storage temp.: Store at -20°C
• solubility: DMSO:47.33(Max Conc. mg/mL);114.08(Max Conc. mM); DMF:30.0(Max Conc. mg/mL);72.31(Max Conc. mM); Ethanol:56.0(Max Conc. mg/mL);134.98(Max Conc. mM); Ethanol:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.48(Max Conc. mM)
• form: A crystalline solid
• pka: 5.24±0.10(Predicted)
• color: White to khaki
• 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: C(NOC)(=O)C1=CC=CC=C1NC1C(Cl)=CN=C(NC2N(C(C)C)N=C(C)C=2)C=1

Description and Uses

GSK2256098 is an inhibitor of focal adhesion kinase (FAK). It is selective for FAK, inhibiting only FAK greater than 50% in a panel of 261 kinases. GSK2256098 inhibits FAK autophosphorylation at tyrosine 397 (Y397) in OVCAR8 ovarian, U87MG glioblastoma, and A549 lung cancer cell lines (IC₅₀s = 15, 8.5, and 12 nM, respectively). It induces apoptosis and increases PARP levels, decreases viability (IC₅₀ = 25 μM), and inhibits colony formation in L3.6P1 cells. GSK2256098 (75 mg/kg per day) also leads to lower tumor weight and fewer metastases in the Ishikawa orthotopic mouse model of uterine cancer.

GSK 2256098 is FAK inhibitor. It can be used in biological study of molecular pathways: endothelial cell FAK-?A target for cancer treatment.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H332-H335
• Precautionary statements: P280-P305+P351+P338-P310