USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
USD $9.00-99.00 / Kilogram
vemurafenib (plx4032, rg7204; ro5185426) is a novel and potent inhibitor of b-rafv600e with ic50 of 31 nm.
ic50 value: 31 nm(b-rafv600e); 48 nm (c-raf )[1]
target: b-rafv600e
target: plx4032 inhibits b-rafv600e, c-raf, as well as wildtype b-raf, with ic50 of 31 nm, 48 nm and 100 nm, respectively. plx4032 also inhibits several non-raf kinases, including ack1, khs1, and srms, with ic50 of 18 nm to 51 nm [1]. in melanoma cell lines, the inhibitory effect by plx4032 depends on b-raf mutational status, because plx4032 potently inhibits those harboring b-raf v600 mutants, including v600e, v600d, v600k, and v600r, but not wildtype or other mutants. the ic50 values of plx4032 on these cells, including malme-3m, colo829, colo38, a375, sk-mel28, and a2058, ranges from 20 nm to 1 μm. in these cells, plx4032 (0.1 μm to 30 μm) also inhibits the phosphorylation of both mek1/2 and erk1/2 [2]. plx4032 is highly effective in the treatment of melanoma, for its ability of inhibiting b-rafv600e. however, plx4032 displays limited effect in colon cancer patients that also carrying b-rafv600e oncoprotein. the reason for this is that, in colon cancer cells, b-rafv600e inhibition by plx4032 results in a rapid feedback egfr activation, which compensates for the plx4032-inhibited cell proliferation [3].
in vivo: in b-rafv600e-mutant mice xenograft models, plx4032 (6 mg/kg–20 mg/kg) inhibits tumor growth [1]. in mice xenograft models of lox, colo829, and a375 cells, plx4032 (12.5 mg/kg–100 mg/kg) inhibits tumor growth and prolongs mice survival [2].