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CEP-32496

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    CEP-32496
  • CEP-32496
Cat No: 18776
Biochemicals - Kinase Inhibitors
Cayman

B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} CEP-32496 is a potent...

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Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • N-?[3-?[(6,?7-?dimethoxy-?4-?quinazolinyl)?oxy]?phenyl]?-?N'-?[5-?(2,?2,?2-?trifluoro-?1,?1-?dimethylethyl)?-?3-?isoxazolyl]?-urea
Correlated keywords:
  • CEP32496 mutation mutant BRaf B-Raf BRAFV600E BRAF-V600E A-375 Colo205 pMEK pERK p-MEK P-ERK Val-600
Product Overview:
B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling.{27148} Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi.{27148} CEP-32496 is a potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay).{30907} It blocks B-RafV600E-dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50s = 78 and 60 nM, respectively).{30907} CEP-32496 binds kinases other than B-Raf but displays selective cytotoxicity for cells expressing B-RafV600E.{30907} It displays good oral bioavailability in rats, dogs, and monkeys and has single oral dose pharmacodynamics inhibition of both pMEK and pERK in B-RafV600E colon carcinoma xenografts in nude mice.{30907}
Size 500 µg
Shipping dry ice
CAS Number 1188910-76-0
Molecular Formula C24H22F3N5O5
SMILES COC1=C(OC)C=C(C(OC2=CC=CC(NC(NC3=NOC(C(C)(C)C(F)(F)F)=C3)=O)=C2)=NC=N4)C4=C1
Molecular Weight 517,5
Formulation A crystalline solid
Purity ≥95%
Custom Code 2933.59
UNSPSC code 12352100

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Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

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