| 产品详情 |
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| Product Name | CEP-32496 |
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| Description | Purity >95%. B-Raf is a MAP kinase kinase kinase, which functions downstream of Ras family GTPases to activate MEK1/2 and ERK1/2 signaling. Mutations of B-Raf, particularly at Val600, are common in melanomas and melanocytic nevi. CEP-32496 is a potent inhibitor of B-RafV600E (Kd = 14 nM in an in vitro binding assay). It blocks B-RafV600E -dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC50 s = 78 and 60 nM, respectively). CEP-32496 binds kinases other than B-Raf but displays selective cytotoxicity for cells expressing B-RafV600E . 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. |
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| Size | n/a |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | N-[3-[(6,7-dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-urea |
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| Gene, Accession, CAS # | CAS: 1188910-76-0 |
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| Catalog # | LS-H7070 |
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| Order / More Info | CEP-32496 from LIFESPAN BIOSCIENCES INC. |
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| Product Specific References | n/a |
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