FRAX 597

• Supplier: Tocris Bioscience
• Catalog: 5190
• Prices: $205.00, $865.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1286739-19-2
• 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
• Formula: C29H28ClN7OS
• Molecular Weight: 558.1
• Purity: >98 %
• Description: Potent group I PAK inhibitor (IC 50 values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). Exhibits significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC 50 >10 μ M for PAK4). Inhibits proliferation of pancreatic cancer and schwannoma cells in vitro and exhibits antitumor effects in mice.

Product References

Proteinase-activated receptor 2 sensitizes transient receptor potential vanilloid - Proteinase-activated receptor 2 sensitizes transient receptor potential vanilloid

Chen Y, Yang C, Wang ZJ. Neuroscience. 2011 Oct 13;193:440-51.

Tryptase/Protease-activated receptor 2 interactions induce selective - Tryptase/Protease-activated receptor 2 interactions induce selective

McLarty JL, Melendez GC, Brower GL, Janicki JS, Levick SP. Hypertension. 2011 Aug;58(2):264-70.

Involvement of serine protease and proteinase-activated receptor 2 in - Involvement of serine protease and proteinase-activated receptor 2 in

Andoh T, Takayama Y, Yamakoshi T, Lee JB, Sano A, Shimizu T, Kuraishi Y. J Pharmacol Exp Ther. 2012 Oct;343(1):91-6.