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FRAX486

Chemical Structure : FRAX486

CAS No.: 1232030-35-1

FRAX486 (FRAX-486)

Catalog No.: PC-73199Not For Human Use, Lab Use Only.

FRAX486 is potent, selective, brain-penetrant group I PAKs inhibitor with IC50 of 8.25, 39.5, and 55.3 nM for PAK1, PAK2 and PAK3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

FRAX486 is potent, selective, brain-penetrant group I PAKs inhibitor with IC50 of 8.25, 39.5, and 55.3 nM for PAK1, PAK2 and PAK3, respectively.
FRAX486 poorly inhibits group II PAK (PAK4) with IC50 of 779 nM.
FRAX486 rescued increased density of apical dendritic spines, reversed hyperactivity and repetitive behaviors in Fmr1 KO mice.
FRAX486 ameliorateed adolescent synapse loss in the prefrontal cortex and adult behavior change in a DISC1 knockdown mouse model.
FRAX486 combined with midostaurin significantly prolonged leukemia progression-free survival in FLT3 D835H PDX-ALL model.

Physicochemical Properties

M.Wt 513.4
Formula C25H23Cl2FN6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(2,4-Dichlorophenyl)-8-ethyl-2-[[3-fluoro-4-(1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one

References

1. Hayashi-Takagi A, et al. Proc Natl Acad Sci U S A. 2014 Apr 29;111(17):6461-6.

2. Dolan BM, et al. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5671-6.

3. Wang Y, et al. PLoS One. 2016 Apr 12;11(4):e0153312.

4. Siekmann IK, et al. Blood Adv. 2018 Oct 9;2(19):2554-2567.

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