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PLX-4720
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PLX-4720图片
CAS NO:918505-84-7
规格:98%
分子量:413.83
包装与价格:
包装价格(元)
10mg电议
25mg电议
100mg电议

产品介绍
BRAF kinase inhibitor
CAS:918505-84-7
分子式:C17H14ClF2N3O3S
分子量:413.83
纯度:98%
存储:Store at -20°C

Background:

PLX-4720, a 7-azaindole derivative discovered by a structure-guided discovery approach, is a potent inhibitor of B-RafV600E, the most frequent oncogenic protein kinase mutation, with the value of 50% inhibition concentration IC50of 13 nM. PLX-4720 exhibits selective inhibition against B-RafV600Erather than wild type B-Raf (IC50= 160 nM) as well as a wide range of other kinases, such as FRK, CSK, SRC, FAK, FGFR, and Aurora A (IC50> 1000 nM for all). 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.


Reference


[1].Tsai J, Lee JT, Wang W, Zhang J, Cho H, Mamo S, Bremer R, Gillette S, Kong J, Haass NK, Sproesser K, Li L, Smalley KS, Fong D, Zhu YL, Marimuthu A, Nguyen H, Lam B, Liu J, Cheung I, Rice J, Suzuki Y, Luu C, Settachatgul C, Shellooe R, Cantwell J, Kim SH, Schlessinger J, Zhang KY, West BL, Powell B, Habets G, Zhang C, Ibrahim PN, Hirth P, Artis DR, Herlyn M, Bollag G. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A. 2008 Feb 26;105(8):3041-3046