FRAX486

FRAX486 is an inhibitor of group I p21-activated kinases (PAKs, IC50s = 8.25, 39.5, and 55.3 nM for PAK1, PAK2, and PAK3, respectively). It is selective for group I PAKs over PAK4, a group II PAK (IC50 = 779 nM). FRAX486 (20 mg/kg) reverses decreases in the mean density of apical dendritic spines in the temporal cortex in the Fmr1-/- mouse model of fragile X syndrome. It completely abolishes audiogenic seizures, hyperactivity, and stereotypical movements in Fmr1-/- mice when administered at a dose of 30 mg/kg. FRAX486 prevents adolescent cortical dendritic spine loss and rescues prepulse inhibition deficits in a Disc1 knockdown mouse model of schizophrenia.Formal Name: 6-(2,4-dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one. CAS Number: 1232030-35-1. Molecular Formula: C25H23Cl2FN6O. Formula Weight: 513.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml, Ethanol: slight sol. lambdamax: 215, 269, 307, 370 nm. SMILES: ClC1=CC(Cl)=C(C2=CC3=CN=C(NC4=CC(F)=C(N5CCNCC5)C=C4)N=C3N(CC)C2=O)C=C1. InChi Code: InChI=1S/C25H23Cl2FN6O/c1-2-34-23-15(11-19(24(34)35)18-5-3-16(26)12-20(18)27)14-30-25(32-23)31-17-4-6-22(21(28)13-17)33-9-7-29-8-10-33/h3-6,11-14,29H,2,7-10H2,1H3,(H,30,31,32). InChi Key: DHKFOIHIUYFSOF-UHFFFAOYSA-N.