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CEP-32496 hydrochloride
Cat No.
CEI-1274
Description
CEP-32496 hydrochloride is a highly potent inhibitor of wild-type BRAF, V600E mutant BRAF and c-Raf with Kd values of 14 nM, 36 nM and 39 nM, respectively.
Product Overview
CEP-32496 is a selective inhibitor of BRAFV600E with IC50 value of 669 nM. BRAF is a member of Raf kinase family and plays an important role in sending signals (directing cell growth) inside cells. BRAF involves in regulating MAP kinase/ERKs signaling pathway and mutant BRAFV600E activates MAPK pathway, it has been shown that BRAF mutant BRAFV600E is correlated with several human cancers. CEP-32496 is a potent BRAFV600E inhibitor and has a different selectivity with the reported BRAFV600E inhibitor RG7204. Using Ambit Kinomescan Assay, it was shown that CEP-32496 potently binding to RAF family with Kd value ranged from 14 to 39 nmol/L. When tested with a panel of BRAF mutant (A375, SK-MEL-28, Colo-679, HT-144, and Colon-205) cell lines, CEP-32496 showed a selective cytotoxicity profile against tumor cell lines with V600E mutant while had no effect on wild type cell lines (HCT116, Hs578T, LNCaP, DU145, PC-3). CEP-32496 treatment exhibited high cytotoxicity against human tumor cell lines with expression of BRAFV600E while had little effect on wild type BRAF expressed cell lines. In nude mice model with Colo-205 tumor cells subcutaneous xenograft, oral administration of CEP-32496 significantly inhibited pMEK normalization, induced tumor stasis (40%) while control group did not have this phenomenon in a dose of 30 mg/kg. CEP-32496 also inhibits MEK phosphorylation with IC 50 value of 60 nM.
CAS No.
1227678-26-3
Molecular Weight
553.92
Purity
0.98
Storage
Store at -20°C
Synonyms
CEP 32496 hydrochloride; CEP32496 hydrochloride
Targets
B-Raf/C-Raf
IC50
14 nM (Kd); 36 nM (Kd); 39 nM (Kd)
Molecular Formula
C24H23ClF3N5O5
Chemical Name
1-[3-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea; hydrochloride
Solubility
DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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