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维罗非尼Vemurafenib (PLX4032; RG7204) 是有效的 B-RAF 抑制剂,能够抑制 RAFV600E 和 c-RAF-1 的活性,IC50 分别为 31 nM 和 48 nM。
物化属性:
密度:1.818
熔点:112-114 °C
折射率:1.645
PSA:90.82000
LOGP:2.93060
[1]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.
[2]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527.
[3]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103.
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