Product Name

Vemurafenib

General description

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

Synonym

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

Purity

≥98%(HPLC)

CAS Number

918504-65-1

Formula

C²³H¹⁸ClF²N³O³S

Molecular Weight

489.922

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White or Off-white or light grey solid

Solubility(25℃)

DMSO

≥50mg/mL

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol   Actions

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.

Application

1. Antineoplastic Agents

2. Enzyme Inhibitors

l  Packaging & Storage

Packaging

10mg; 50mg; 250mg

Storage temp.

0-5℃

l  Precautions and Disclaimer

This   product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov