Vemurafenib（维罗非尼）又称为PLX4032、RO5185426、RG7204，是一种新型、有效的B-RafV600E抑制剂（IC50=31 nM），并作用于C-Raf、MAP4K5 (KHS1)、SRMS、ACK1、FGR，IC50分别为48 nM、51 nM、18 nM、19 nM、63 nM。Vemurafenib显著抑制B-RafV600E突变的黑色素瘤细胞增殖，抑制ERK和MEK磷酸化，并抑制B-RafV600E移植瘤小鼠中的肿瘤生长。

参考文献

[1]Halaban R, et al. PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells. Pigment Cell Melanoma Res. 23: 190-200 (2010).

[2]Tap WD, et al. Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma. Neoplasia 12: 637-649 (2010).

[3]Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 467: 596-599 (2010).

[4]Lee JT, et al. PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas.  Pigment Cell Melanoma Res. 23: 820-827 (2010).

[5] Yang H, et al. RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models. Cancer Res, 70(13): 5518-5527 (2010).

[6] Bollag G, et al.Vemurafenib: the first drug approved for BRAF-mutant cancer. Nature Reviews Drug Discovery 11: 873-886 (2012).

[7] Yang H, et al.Antitumor Activity of BRAF Inhibitor Vemurafenib in Preclinical Models of BRAF-Mutant Colorectal Cancer.  Cancer Res, 72(3): 779-789 (2012).

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