Synonym: 6-(2,4-Dichlorophenyl)-8-ethyl-2-(3-fluoro-4-(piperazin-1-yl)phenylamino)pyrido[2,3-d] pyrimidin-7(8H)-one; 6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one; FRAX 486; FRAX-486
CAS Number: 1232030-35-1
Empirical Formula (Hill Notation): C25H23Cl2FN6O
Molecular Weight: 513.39
MDL Number: MFCD26793866
Linear Formula: C25H23Cl2FN6O
Product Type: Chemical
assay |
≥98% (HPLC) |
color |
white to beige |
form |
powder |
SMILES string |
FC1=CC(NC2=NC(N3CC)=C(C=N2)C=C(C4=CC=C(C=C4Cl)Cl)C3=O)=CC=C1N5CCNCC5 |
solubility |
DMSO: 2 mg/mL, clear |
storage temp. |
−20°C |
Biochem/physiol Actions: |
FRAX486 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/2/3 IC50 = 8.25/39.5/55.3 nM; group II PAK4 IC50 = 779 nM). FRAX486 effectively inhibits PAK-mediated PKD1 Ser203 phosphorylation and PAK1/2 Ser144/141 autophosphorylation upon angiotensin II (ANGII) stimulation of rat IEC-18 cells (IC50 ∼0.5 μM) and exhibits in vivo efficacy in rescuing the autism-like phenotypes among Fmr1 knockout fragile syndrome (FXS) mice (20 mg/kg s.c.) as well as in ameliorating schizophrenia-associated dendritic spine deterioration among Disc1 knockdown mice (10 μg/g or 10 mg/kg i.p.) with good pharmacokinetic properties and blood–brain barrier (BBB) permeability. |
RIDADR |
NONH for all modes of transport |
WGK Germany |
WGK 3 |
Flash Point(F) |
Not applicable |
Flash Point(C) |
Not applicable |
Purity |
≥98% (HPLC) |
Storage Temp. |
−20°C |
UNSPSC |
12352200 |