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| | GSK-2256098 Basic information |
| Product Name: | GSK-2256098 | | Synonyms: | GSK-2256098;2-(5-chloro-2-(1-isopropyl-3-methyl-1H-pyrazol-5-ylamino)pyridin-4-ylamino)-N-methoxybenzamide;GTPL7939;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;CS-2424;FAK inhibitor GS2256098;GSK-2256098;GSK 2256098 | | CAS: | 1224887-10-8 | | MF: | C20H23ClN6O2 | | MW: | 414.89 | | EINECS: | | | Product Categories: | Inhibitors;APIs | | Mol File: | 1224887-10-8.mol |  |
| | GSK-2256098 Chemical 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) | | 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 |
| | GSK-2256098 Usage And Synthesis |
| Description | 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. | | 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 |
| | GSK-2256098 Preparation Products And Raw materials |
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