CEP-32496 (free base)

CEP-32496 (free base) 化学特性,用途語,生産方法

• 説明

  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-Raf^V600E (K_d = 14 nM in an in vitro binding assay). It blocks B-Raf^V600E-dependent phosphorylation of MEK in human melanoma A375 and colorectal cancer COLO 205 cells (IC₅₀s = 78 and 60 nM, respectively). CEP-32496 binds kinases other than B-Raf but displays selective cytotoxicity for cells expressing B-Raf^V600E. It displays good oral bioavailability in rats, dogs, and monkeys and has single oral dose pharmacodynamics inhibition of both pMEK and pERK in B-Raf^V600E colon carcinoma xenografts in nude mice.

• 使用

  CEP 32496 is an orally active BRAFV600E inhibitor with selective cellular and in vivo antitumor activity.

CEP-32496 (free base) 上流と下流の製品情報

CEP-32496 (free base) 生産企業

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CEP-32496 (free base) スペクトルデータ(¹HNMR)

1188910-76-0, CEP-32496 (free base) キーワード