FRAX597 ( FRAX597; FRAX-597; FRAX 597 )

Catalog No. M17238 CAS No. 1286739-19-2

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Product Name

FRAX597
Note

Research use only, not for human use.
Brief Description

FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM).
Description

FRAX597 is a potent and selective inhibitor of the p21-activated kinases. FRAX597 inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. FRAX597 inhibits the proliferation of NF2-deficient schwannoma cells in culture and displayed potent anti-tumor activity in vivo, impairing schwannoma development in an orthotopic model of NF2. These studies identify a novel class of orally available ATP-competitive Group I PAK inhibitors with significant potential for the treatment of NF2 and other cancers.
Synonyms

FRAX597; FRAX-597; FRAX 597
Pathway

Angiogenesis
Target

EGFR
Recptor

PAK1; PAK2; PAK2; PAK3
Research Area

Cancer
Indication

——

CAS Number

1286739-19-2
Formula Weight

558.1
Molecular Formula

C29H28ClN7OS
Purity

98%
Solubility

DMSO : 14.29 mg/mL. 25.60 mM;H2O : < 0.1 mg/mL
SMILES

CCn1c2nc(ncc2cc(c1=O)c1c(cc(cc1)c1cncs1)Cl)Nc1ccc(cc1)N1CCN(CC1)C
Chemical Name

6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one

1. Licciulli S, et al. J Biol Chem. 2013, 288(4), 29105-29114.

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