产品说明书

PLX7904

Print
Chemical Structure| 1393465-84-3 同义名 : PB04
CAS号 : 1393465-84-3
货号 : A605818
分子式 : C24H22F2N6O3S
纯度 : 98+%
分子量 : 512.532
MDL号 : MFCD29472265
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(58.53 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Raf
描述 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.95mL

0.39mL

0.20mL

9.76mL

1.95mL

0.98mL

19.51mL

3.90mL

1.95mL
参考文献

[1]Zhang C, et al. RAF inhibitors that evade paradoxical MAPK pathway activation. Nature. 2015 Oct 22;526(7574):583-586.

[2]Basile KJ, et al. Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors. Pigment Cell Melanoma Res. 2014 May;27(3):479-84

[3]Le K, et al. Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cells. Pigment Cell Melanoma Res. 2013 Jul;26(4):509-17