FRAX597 | B1890

FRAX597 is a potent group I PAK (p21-activated kinase) inhibitor (IC₅₀ values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). Displays significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC₅₀ >10 μM for PAK4). FRAX597 inhibits the proliferation of NF2-deficient schwannoma cells in culture and displays potent anti-tumor activity in vivo.

FRAX597 is a potent group I PAK (p21-activated kinase) inhibitor (IC₅₀ values are 8, 13 and 19 nM for PAK1, 2 and 3, respectively). Displays significant inhibition of YES1, RET, CSF1R and TEK at 100 nM, but is inactive against group II PAK isoforms (IC₅₀ >10 μM for PAK4). FRAX597 inhibits the proliferation of NF2-deficient schwannoma cells in culture and displays potent anti-tumor activity in vivo.

B1890 | FRAX597 DataSheet

Alternate Name/Synonyms: 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

Appearance: Yellow solid

Formulation: N/A

CAS Number: 1286739-19-2

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₉H₂₈ClN₇OS

Molecular Weight: 558.1

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (>5 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent group I PAK (p21-activated kinase) inhibitor

MDL Number: N/A

PubChem CID: 70934541

SMILES: CCN1C2=NC(=NC=C2C=C(C1=O)C3=C(C=C(C=C3)C4=CN=CS4)Cl)NC5=CC=C(C=C5)N6CCN(CC6)C

InChi: InChI=1S/C29H28ClN7OS/c1-3-37-27-20(14-24(28(37)38)23-9-4-19(15-25(23)30)26-17-31-18-39-26)16-32-29(34-27)33-21-5-7-22(8-6-21)36-12-10-35(2)11-13-36/h4-9,14-18H,3,10-13H2,1-2H3,(H,32,33,34)

InChi Key: DHUJCQOUWQMVCG-UHFFFAOYSA-N