[sun-shine]

PLX-4720;
CAS#918505-84-7;
purity:98%;
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Biological Activity of PLX-4720:
PLX4720, a 7-azaindole derivative that inhibits B-RafV600E with an IC50 of 13 nM, defines a class of kinase inhibitor with marked selectivity in both biochemical and cellular assays. PLX4720 preferentially inhibits the active B-RafV600E kinase compared with a broad spectrum of other kinases (IC50:B-Raf=160 nM, BRK=130 nM, other kinases >1000nM), and potent cytotoxic effects are also exclusive to cells bearing the V600E allele (GI50<1.7 μM, while other wild cell GI50>10μM). [1]
Consistent with the high degree of selectivity, ERK phosphorylation is potently inhibited by PLX4720 in B-RafV600E -bearing tumor cell lines but not in cells lacking oncogenic B-Raf. [1]
In B-RafV600E -dependent tumor xenograft models, orally dosed PLX4720 causes significant tumor growth delays, including tumor regressions, without evidence of toxicity. [1]

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References on PLX-4720:
[1] Caroline M. Emery et al. Proc Natl Acad Sci U S A. 2009 December 1;106(48):20411–20416

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