产品名称

维罗菲尼(Vemurafenib)

一般描述

Vemurafenib(维罗菲尼)  is an orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity.

别 称

N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide;  Zelboraf; PLX4032; PLX-4032

纯 度

≥98%(HPLC)

CAS NO.

918504-65-1

分子式

C²³H¹⁸ClF²N³O³S

分子量

489.922

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色或类白色或浅灰色固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Vemurafenib is an orally bioavailable,  ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase with potential antineoplastic activity. Vemurafenib selectively binds to the  ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E); the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors, including melanoma, colorectal, thyroid and other cancers.

l  包装与存储

包 装

10mg; 50mg; 250mg

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov