Product Name: CEP-32496
 CAT#: A-1310

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 Synonym:CEP-32496

CEP-32496 Chemical Structure
CEP-32496 chemical structure


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IUPAC/Chemical name: 1-[3-(6,7-Dimethoxyquinazolin-4-yl)oxyphenyl]-3-[5-(2,2,2-trifluoro-1,1- dimethylethyl)isoxazol-3-yl]urea

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Biological Activity
CEP-32496 is a potent BRAF inhibitor in an in vitro binding assay for mutated BRAF(V600E) (K(d) BRAF(V600E) = 14 nmol/L) and in a mitogen-activated protein (MAP)/extracellular signal-regulated (ER) kinase (MEK) phosphorylation (pMEK) inhibition assay in human melanoma (A375) and colorectal cancer (Colo-205) cell lines (IC(50) = 78 and 60 nmol/L). CEP-32496 is orally bioavailable in multiple preclinical species (>95% in rats, dogs, and monkeys) and has single oral dose pharmacodynamic inhibition (10-55 mg/kg) of both pMEK and pERK in BRAF(V600E) colon carcinoma xenografts in nude mice. Sustained tumor stasis and regressions are observed with oral administration (30-100 mg/kg twice daily) against BRAF(V600E) melanoma and colon carcinoma xenografts, with no adverse effects. Little or no epithelial hyperplasia was observed in rodents and primates with prolonged oral administration and sustained exposure. CEP-32496 represents a novel and pharmacologically active BRAF inhibitor with a favorable side effect profile currently in clinical development.
Technical Data

Mol. Formula: C24H22F3N5O5
MW: 553.92
CAS#: 1188910-76-0
Purity: >99%
CEP-32496 MSDS CEP-32496 CoA

Reference







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