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-Raf^V600E, the most frequent oncogenic protein kinase mutation, with the value of 50% inhibition concentration IC₅₀of 13 nM. PLX-4720 exhibits selective inhibition against B-Raf^V600Erather 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-Raf^V600E, induces cell cycle arrest and apoptosis in B-Raf^V600E-positive melanoma cells and causes tumor growth delays in B-Raf^V600E-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