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GSK-2256098

Chemical Structure : GSK-2256098

CAS No.: 1224887-10-8

GSK-2256098 (GTPL-7939;GSK2256098;GTPL7939)

Catalog No.: PC-42177Not For Human Use, Lab Use Only.

GSK-2256098 (GTPL-7939) is a potent, selective, reversible and ATP-competitive inhibitor of FAK kinase with Ki of 0.4 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK-2256098 (GTPL-7939) is a potent, selective, reversible and ATP-competitive inhibitor of FAK kinase with Ki of 0.4 nM; dispalys high selectivity over a panel of 261 kinases, including the nearest FAK family member, Pyk2 (>1,000-fold); inhibits FAK activity through targeting the phosphorylation site of FAK Y397; decreases levels of phosphorylated Akt and ERK, cell viability, anchorage-independent growth, and motility in L3.6P1 cells; causes lower microvessel density, less cellular proliferation, and higher apoptosis rates in the Ishikawa model.

Pancreatic Cancer

Phase 2 Clinical

Physicochemical Properties

M.Wt 414.8886
Formula C20H23ClN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

Benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino]-4-pyridinyl]amino]-N-methoxy-

References

1. Zhang J, et al. Cell Cycle. 2014;13(19):3143-9.

2. Soria JC, et al. Ann Oncol. 2016 Dec;27(12):2268-2274.

3. Thanapprapasr D, et al. Mol Cancer Ther. 2015 Jun;14(6):1466-1475.

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