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Biological Activity:
Selective inhibitor of protein kinase, targeting B-Raf (V600E) (IC50: 44 nM); PLX4032 has been shown to cause programmed cell death in melanoma cell lines; a potential anti-tumor agent under clinical trials.
References:
G Bollag et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 2010, 467, 596–599. [online]
PI Poulikakos et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010, 464, 427-430. [online]
E Sala et al. BRAF Silencing by Short Hairpin RNA or Chemical Blockade by PLX4032 Leads to Different Responses in Melanoma and Thyroid Carcinoma Cells. Mol. Cancer Res. 2008, 6(5), 751-759. [online]
Chemical Name: N-[2,4-Difluoro-3-[[5-(3-pyridinyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]phenyl]-2-propanesulfonamide
PLX 4032 | B-Raf inhibitor | Axon Medchem | Axon 1624 | Vemurafenib - RG7204 - PLX4032 - RG 7204 - RO5184226 - Ro 5185426 |