GSK-2256098
- CAS NO.:1224887-10-8
- Empirical Formula: C20H23ClN6O2
- Molecular Weight: 414.89
- MDL number: MFCD30502650
- Update Date: 2024-11-07 21:39:59
What is GSK-2256098?
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.
The Uses of GSK-2256098
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
Properties of GSK-2256098
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) |
Safety information for GSK-2256098
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H332:Acute toxicity,inhalation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P310:Immediately call a POISON CENTER or doctor/physician. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for GSK-2256098
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 |
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