FRAX597

FRAX597 is an inhibitor of p21-activated kinase (PAK) that is selective for group I PAKs (IC50s = 7.7, 12.8, and 19.3 nM for PAK 1, 2, and 3, respectively) over group II PAKs (IC50 > 10 µM for PAK4 and 50 = 70 nM), prevents proliferation of transformed Schwann cells by halting the cell cycle in the G1 phase, and reduces the growth of schwannoma mouse xenografts. It also reduces proliferation and survival in ovarian and pancreatic cancer cells and works synergistically with gemcitabine (Cay-11690) in pancreatic cancer models in vitro and in vivo.Formal 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. CAS Number: 1286739-19-2. Molecular Formula: C29H28ClN7OS. Formula Weight: 558.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 14 mg/ml, DMSO: 11 mg/ml, Ethanol: 0.1 mg/ml. lambdamax: 216, 272, 374 nm. SMILES: CN1CCN(C2=CC=C(NC3=NC=C(C=C(C4=C(Cl)C=C(C5=CN=CS5)C=C4)C(N6CC)=O)C6=N3)C=C2)CC1. InChi Code: InChI=1S/C29H28ClN7OS/c1-3-37-27-20(14-24(28(37)38)23-9-4-19(15-25(23)30)26-17-31-18-39-26)16-32-29(34-27)33-21-5-7-22(8-6-21)36-12-10-35(2)11-13-36/h4-9,14-18H,3,10-13H2,1-2H3,(H,32,33,34). InChi Key: DHUJCQOUWQMVCG-UHFFFAOYSA-N.