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Description: PLX4720 (PLX-4720; PLX 4720), a 7-azaindole/pyrrolopyridine-based vemurafenib derivative discovered by a structure-guided discovery approach, is a novel, potent and selective inhibitor of B-RafV600E mutant with potential antitumor activity. It inhibits B-RafV600E with an IC50 of 13 nM in a cell-free assay, and is 10-fold more selective for B-RafV600E over wild-type B-Raf. PLX-4720 potently inhibits ERK phosphorylation in tumor cell lines harboring B-RafV600E, induces cell cycle arrest and apoptosis in B-RafV600E-positive melanoma cells and causes tumor growth delays in B-RafV600E-dependent tumor xenograft models through oral administration.
References: Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6.
Product Catalog 2022
Guide to Product Handling
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
Purity ≥98%
COA
MSDS
Antimetastatic effects of PLX4720 require NK cells. Cancer Res; 74(24); 7298–308, 2014
PLX4720 requires perforin and CD226 for optimal antimetastatic activity.
qPCR analysis showing that PLX4720 (3μM) alters the expression of XBP1s mRNA.