A FAK inhibitor
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GSK2256098

Item No. 22955

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy-benzamide
CAS Number
1224887-10-8
Molecular Formula
C20H23ClN6O2
Formula Weight
414.9
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
224, 252, 288 nm
SMILES
O=C(NOC)C1=CC=CC=C1NC2=CC(NC3=CC(C)=NN3C(C)C)=NC=C2Cl
InChi Code
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)
InChi Key
BVAHPPKGOOJSPU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $38

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    5 mg

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    10 mg

    $255

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    25 mg

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    Product 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, J., He, D.H., Zajack-Kaye, M., et al. A small molecule FAK kinase inhibitor, GSK2256098, inhibits growth and survival of pancreatic ductal adenocarcinoma cells. Cell Cycle 13(19), 3143-3149 (2014).

    2. Thanapprapasr, D., Previs, R.A., Hu, W., et al. PTEN expression as a predictor of response to focal adhesion kinase inhibition in uterine cancer. Mol. Cancer. Ther. 14(16), 1466-1475 (2015).