PLX7904 是有效的，选择性的 BRAF 抑制剂，在表达

PLX7904 is a potent and selective BRAF inhibitor, with IC₅₀ of appr 5 nM against BRAF^V600E in mutant RAS expressing cells.

PLX7904 inhibits the in vitro growth of two melanoma cell lines (A375 and COLO829) and an additional human colorectal cancer cell line COLO205 that expresses BRAF^V600E with IC₅₀ values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively, on a par with vemurafenib IC₅₀ values in the same assays (0.33 μM, 0.69 μM, and 0.25 μM, respectively)^[1]. PLX7904 and PLX8394 potently inhibit ERK1/2-driven GAL4-Elk1 reporter activity in PRT cells as well as parental cells. PLX7904 and PLX8394 treatment at 1 μM concentration reduce colony formation and viability in parental cells to a similar level as PLX4720^[2]. PPLX7904 potently inhibits phosphorylation of ERK1/2 in mutant BRAF melanoma cells without eliciting paradoxical activation in wild-type BRAF, mutant NRAS melanoma cells. PPLX7904 inhibits ERK1/2 in PLX470-resistant cell lines. PPLX7904 treatment promotes apoptosis and inhibits anchorage-independent growth of vemurafenib resistant cells^[3].

512.53

Solid

C₂₄H₂₂F₂N₆O₃S

1393465-84-3

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 30 mg/mL (58.53 mM)

* "≥" means soluble, but saturation unknown.

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
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• 1.

  请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

  Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution

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

  [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 [Content Brief]

  [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 [Content Brief]