A group I PAK inhibitor
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FRAX486

Item No. 24682

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.2 mg/mlEthanol: slight sol
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    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).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dolan, B.M., Duron, S.G., Campbell, D.A., et al. Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc. Natl. Acad. Sci. USA 110(14), 5671-5676 (2013).

    2. Hayashi-Takagi, A., Araki, Y., Nakamura, M., et al. PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc. Natl. Acad. Sci. USA 111(17), 6461-6466 (2014).