| Identification | Back Directory | [Name]
GSK-2256098 | [CAS]
1224887-10-8 | [Synonyms]
CS-2424
GTPL7939
GSK-2256098
GSK-2256098;GSK 2256098
FAK inhibitor GS2256098
2-(5-chloro-2-(1-isopropyl-3-methyl-1H-pyrazol-5-ylamino)pyridin-4-ylamino)-N-methoxybenzamide
Benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy-
2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino}-4-pyridinyl)amino]-N(methyloxy)benzamide | [Molecular Formula]
C20H23ClN6O2 | [MDL Number]
MFCD30502650 | [MOL File]
1224887-10-8.mol | [Molecular Weight]
414.89 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Description]
GSK2256098 is an inhibitor of focal adhesion kinase (FAK).1 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.2 | [Uses]
GSK 2256098 is FAK inhibitor. It can be used in biological study of molecular pathways: endothelial cell FAK-?A target for cancer treatment. | [storage]
Store at -20°C |
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