FRAX 597
Chemical Name: 6-[2-Chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7-(8H)-one
Purity: ≥98%
Biological Activity
FRAX 597 is a potent group I PAK inhibitor (IC50 values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). FRAX 597 exhibits significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC50 >10 μM for PAK4). FRAX 597 inhibits proliferation of pancreatic cancer and schwannoma cells in vitro and exhibits antitumor effects in mice.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.
Licciulli et al.
J.Biol.Chem., 2013;288:29105 -
FRAX597, a PAK1 inhibitor, synergistically reduces pancreatic cancer growth when combined with gemcit.
Yeo et al.
BMC Cancer, 2016;16:24
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