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PLX-4720

Chemical Structure : PLX-4720

CAS No.: 918505-84-7

PLX-4720 (PLX4720;PLX 4720)

Catalog No.: PC-45918Not For Human Use, Lab Use Only.

PLX-4720 (PLX4720 ) is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM.

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Biological Activity

PLX-4720 (PLX4720 ) is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM.
PLX-4720 dispalys 10-fold selectivity over wild-type B-Raf, and remarkably selective against a diverse panel of 70 other kinases.
PLX-4720 inhibits ERK phosphorylation in COLO25 cells with IC50 of 14 nM.
PLX-4720 induces cell cycle arrest and apoptosis exclusively in B-Raf(V600E)-positive cells.
PLX-4720 inhibits tumor growth in B-Raf(V600E)-dependent tumor xenograft models; orally active.

Physicochemical Properties

M.Wt 413.8262
Formula C17H14ClF2N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-Propanesulfonamide, N-[3-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-

References

1. Tsai J, et al. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-6.

2. Hatzivassiliou G, et al. Nature. 2010 Mar 18;464(7287):431-5.

3. Jiang CC, et al. Clin Cancer Res. 2011 Feb 15;17(4):721-30.

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