PLX4032 (Vemurafenib) is an 7-azaindole-based, orally-available, inhibitor of the B-Raf V600E mutation with

an IC50 of 30 nM. [1] In preclinical tumor models, PLX4032 induces antiproliferative effects in both

mealonama and thyroid cell lines, with a simultaneous dose-dependent block of MEK1/2 phosphorylation.

[1] Apoptosis is also observed in melanoma cell lines upon treatment with PLX4032. Important to note is that

proliferation was inhibited in tumor cell lines expressing B-Raf V600E only, and not B-Raf WT or other B-Raf

mutations. [2]

PLX4032 has marginal effect on cell-cycle arrest, apoptotic cell changes, or alteration of phosphorylated

signaling molecules in lymphocytes. T-cell function was preserved up to 10 uM of PLX4032, while cytotoxic

activty was maintained up to high concentrations of 50 uM. [3] Such observations suggest that PLX4032 can

be used in combination with immunotherapy strategies.

Chemical Formula:

C₂₃H₁₈ClF₂N₃O₃S

CAS No.:

1029872-54-5, 918504-65-1

Molecular Weight:

489.92

Purity:

> 98%

Appearance:

White

Chemical Name:

N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-

difluorophenyl) propane-1-sulfonamide

Solubility:

Up to 100 mM in DMSO

Synonyms:

PLX-4032, PLX4032, RG7204, RO5185426, Vemurafenib, Zelboraf

Storage:

For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution

at -20^oC.

References