PLX4032 (Vemurafenib) Suppliers and Product Information

PLX4032, also known as Vemurafenib, is a potent inhibitor of B-RafV600E kinase with an IC50 of 31 nM. It is used as an antitumor agent, specifically for the treatment of metastatic melanoma with the BRAFV600E mutation. The compound inhibits cell proliferation and ERK phosphorylation in tumor cell lines expressing BRAFV600E or other mutant BRAF proteins altered at codon 600.

PLX4032 was approved by the FDA in August 2011 for the treatment of patients with metastatic melanoma carrying the BRAFV600E mutation. It is marketed under the brand name Zelboraf. The compound is effective against the growth of tumors bearing the B-Raf V600E mutation and has shown promising results in clinical trials.

Frequently Asked Questions about PLX4032 (Vemurafenib)

Q: What is the mechanism of action of PLX4032?

A: PLX4032 is an ATP-competitive inhibitor of mutant V600E and wild-type B-Raf kinases. It selectively inhibits the proliferation of cells expressing BRAFV600E and other mutant BRAF proteins altered at codon 600.

Q: How should PLX4032 be stored?

A: PLX4032 should be stored at -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.

Q: What is the typical purity of commercially available PLX4032?

A: The purity of commercially available PLX4032 typically ranges from 97% to 99%, depending on the supplier.

Q: Is PLX4032 effective against other types of cancer besides melanoma?

A: While PLX4032 is primarily used for melanoma treatment, its effectiveness in other BRAFV600E-positive cancers, such as colon cancer, has been limited due to rapid feedback EGFR activation in these cells.