PLX7904 is aRaf inhibitor, inhibits the growth of two melanoma cell lines (A375 and COLO829) and human colorectal cancer cell line COLO205 that expressed BRAFV600E with IC50 values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively.
PLX7904 hinders the in vitro proliferation of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 expressing BRAFV600E, with IC50 values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, comparable to the IC50 values of vemurafenib in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively)[1]. PLX7904 and PLX8394 effectively suppress ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. Treatment with PLX7904 and PLX8394 at a concentration of 1 μM reduces colony formation and viability in parental cells to a similar extent as PLX4720[2]. PLX7904 strongly inhibits ERK1/2 phosphorylation in mutant BRAF melanoma cells without inducing paradoxical activation in wild-type BRAF or mutant NRAS melanoma cells. It also inhibits ERK1/2 in PLX470-resistant cell lines. Treatment with PLX7904 promotes apoptosis and suppresses anchorage-independent growth of vemurafenib-resistant cells[3].
体外研究
PLX7904 hinders the in vitro proliferation of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 expressing BRAFV600E, with IC50 values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, comparable to the IC50 values of vemurafenib in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively)[1].
PLX7904 and PLX8394 effectively suppress ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. Treatment with PLX7904 and PLX8394 at a concentration of 1 μM reduces colony formation and viability in parental cells to a similar extent as PLX4720[2].
PLX7904 strongly inhibits ERK1/2 phosphorylation in mutant BRAF melanoma cells without inducing paradoxical activation in wild-type BRAF or mutant NRAS melanoma cells. It also inhibits ERK1/2 in PLX470-resistant cell lines. Treatment with PLX7904 promotes apoptosis and suppresses anchorage-independent growth of vemurafenib-resistant cells[3].
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