Vemurafenib (PLX4032)

  Cat. No.:  DC1071   Featured
Chemical Structure
918504-65-1
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More than 5000 active chemicals with high quality for research!
Field of application
PLX4032 (Vemurafenib, RG7204, Zelboraf, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.
Cas No.: 918504-65-1
Chemical Name: RG7204,PLX-4032,PLX 4032,RG-7204
Synonyms: RG7204,PLX-4032,PLX 4032,RG-7204
SMILES: FC1=CC=C(C(F)=C1C(C2=CNC3=NC=C(C=C32)C4=CC=C(C=C4)Cl)=O)NS(CCC)(=O)=O
Formula: C23H18ClF2N3O3S
M.Wt: 489.92
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Vemurafenib is a novel and potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively.
In Vivo: Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2].
In Vitro: Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC5049 RAF265 (CHIR-265) RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.
DC6301 PLX-4720 PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
DC1071 Vemurafenib (PLX4032) PLX4032 (Vemurafenib, RG7204, Zelboraf, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.
DC8344 LY3009120 LY3009120 is a potent and selective pan-RAF inhibitor with potential anticancer activity.
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