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本试剂(维罗非尼)
仅供科研实验使用,不得用于其他用途！
简介：
货 号：LC2-V-2800
名 称：维罗非尼
别 名：Vemurafenib Free Base
C A S ：918504-65-1
分子量：489.92
分子式：C23H18ClF2N3O3S
纯 度：HPLC/TLC:>99%
说 明：Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 100 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 25-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A.
文 献：Vemurafenib inhibited ERK1/2 in the highly sensitive BRAF(V600E/K) cells, while it activated the pathway in the (resistant) BRAF(WT) cells. 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).Using an IC50g cutoff of 1 µM, 13 of 35 cell lines tested showed sensitivity to vemurafenib, 16 were resistant, and 6 were intermediate in sensitivity. Vemurafenib caused growth inhibition, G0/G1 arrest, and apoptosis in the sensitive cell lines. A BRAF mutation favored but did not guarantee a sensitive response, while cells bearing a neuroblastoma RAS viral oncogene homolog mutation or wild-type BRAF were resistant. Tap, W.D., et al. "Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma." Neoplasia 12: 637-649 (2010).Vemurafenib inhibited the growth of B-Raf V600E-positive melanomas in vitro and in vivo. Lee, J.T., 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).Vemurafenib selectively inhibited the RAF/MEK/ERK pathway in BRAF mutant cells and induced regression of BRAF mutant xenografts. However, no tumor regression occurred in patients until greater than 80% inhibition of ERK phosphorylation in the tumors was reached. Bollag, G., et al. "Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma." Nature 467: 596-599 (2010).Treatment of patients with metastatic melanoma that carry the V600E BRAF mutation with vemurafenib resulted in complete or partial tumor regression in the majority of patients. Flaherty, K.T., et al. "Inhibition of mutated, activated BRAF in metastatic melanoma." N. Engl. J. Med. 363: 809-819 (2010).
