SB-590885,405554-55-4

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SB-590885

CAS No. : 405554-55-4

MCE 国际站：SB-590885

产品活性：SB-590885 是一种有效的 B-Raf 抑制剂，K_i 值为 0.16 nM；对其选择性是对 c-Raf 的 11 倍多。

研究领域：MAPK/ERK Pathway

作用靶点：Raf

In Vitro: SB-590885 displays significant selectivity for B-Raf over c-Raf with K_i of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (K_i=38 nM for mutant B-Raf, 6 nM for c-Raf). SB-590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB-590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-Raf^V600E, SB-590885 treatment potently inhibits ERK phosphorylation with EC₅₀ of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC₅₀ of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB-590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. SB-590885 displays high affinity for B-Raf with K_d of 0.3 nM. Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to SB-590885 with IC₅₀ of <1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate SB-590885 resistance in B-Raf V600E-mutated melanomas.

In Vivo: Administration of SB-590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth.

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