Product Information Novel Kinase Inhibitors

for cell signaling & oncology research

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S1152 PLX-4720 (877)796-6397
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» B-Raf
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Technical Data:
Orders
M.Wt: 413.83 F +1-713-922-4115
Formula: C17H14ClF2N3O3S O enquiry@selleckchem.com
Solubility: DMSO O
Cl N S Tech Support
Purity: 99% F H O
tech@selleckchem.com
Storage: at -20℃ 2 years N N
H (chemistry support)
CAS No.: 918505-84-7 techbio@selleckchem.com
(bio support)

Web
Biological Activity
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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
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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]

References Return Policy

[1] Caroline M. Emery et al. Proc Natl Acad Sci U S A. 2009 December 1;106(48):20411–20416 Please inspect packages immediately upon

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