A potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay); blocks B-RafV600E–dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50s = 78 and 60 nM

CEP-32496 – 1 mg

Brand:
Cayman
CAS:
1188910-76-0
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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Description

A potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay); blocks B-RafV600E–dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50s = 78 and 60 nM, respectively); displays good oral bioavailability

Formal name: N-​[3-​[(6,​7-​dimethoxy-​4-​quinazolinyl)​oxy]​phenyl]​-​N’-​[5-​(2,​2,​2-​trifluoro-​1,​1-​dimethylethyl)​-​3-​isoxazolyl]​-urea

Synonyms: 

Molecular weight: 517.5

CAS: 1188910-76-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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