FRAX597

Research use only, not for human use.

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).

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.

FRAX597; FRAX-597; FRAX 597

Angiogenesis

EGFR

PAK1; PAK2; PAK2; PAK3

Cancer

——

1286739-19-2

558.1

C29H28ClN7OS

98%

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

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

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

(-20℃)

With Ice Pack

≥ 2 years