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.
Technical information:
| Chemical Formula: | C23H18ClF2N3O3S | |
| CAS #: | 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 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Yang et al., RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res. 2010, 70, 5518-5527. Pubmed ID: 20551065 |
| 2. | Lee et al., PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas. Pigment Cell Melanoma Res. 2010, 23, 820-827. Pubmed ID: 20973932 |
| 3. | Comin-Anduix et al., The oncogenic BRAF kinase inhibitor PLX4032/RG7204 does not affect the viability or function of human lymphocytes across a wide range of concentrations. Cancer Res. 2010, 16, 6040-6048. Pubmed ID: 21169256 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
