A PAK inhibitor selective for group I PAKs (IC50s = 7.7

FRAX597 – 10 mg

Brand:
Cayman
CAS:
1286739-19-2
Storage:
-20
UN-No:
Non-Hazardous - /

FRAX597 is an inhibitor of p21-activated kinase (PAK) that is selective for group I PAKs (IC50s = 7.7, 12.8, and 19.3 nM for PAK 1, 2, and 3, respectively) over group II PAKs (IC50 > 10 µM for PAK4 and 50 = 70 nM), prevents proliferation of transformed Schwann cells by halting the cell cycle in the G1 phase, and reduces the growth of schwannoma mouse xenografts. It also reduces proliferation and survival in ovarian and pancreatic cancer cells and works synergistically with gemcitabine (Item No. 11690) in pancreatic cancer models in vitro and in vivo.{39133,39132,39134}  

 

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Description

A PAK inhibitor selective for group I PAKs (IC50s = 7.7, 12.8, and 19.3 nM for PAK 1, 2, and 3, respectively) over group II PAKs (IC50 > 10 µM for PAK4 and 50 = 70 nM); reduces proliferation and survival of transformed Schwann cells, ovarian, and pancreatic cells; works synergistically with gemcitabine in pancreatic cancer models in vitro and in vivo,

Formal name: 6-[2-chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-pyrido[2,3-d]pyrimidin-7(8H)-one

Synonyms: 

Molecular weight: 558.1

CAS: 1286739-19-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Signaling

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