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Vemurafenib

产品编号 T2382 CAS 918504-65-1

别名: RO5185426, RG7204, 维罗非尼, PLX4032

Vemurafenib (RG7204) 是一种 B-RAF 抑制剂，可以抑制 RAFV600E 和 c-RAF-1 (IC50=31/48 nM)，具有选择性和有效性。Vemurafenib 具有抗肿瘤活性，用于 BRAF V600E 突变阳性的黑色素瘤治疗。

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Vemurafenib, CAS 918504-65-1

规格	价格/CNY	货期
5 mg	￥ 262	现货
10 mg	￥ 430	现货
25 mg	￥ 690	现货
50 mg	￥ 970	现货
100 mg	￥ 1,491	现货
500 mg	￥ 3,868	现货
1 mL * 10 mM (in DMSO)	￥ 474	现货

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其他形式的 Vemurafenib:

Plx-4032
现货

选择批次

纯度: 99.65%

纯度: 98.4%

纯度: 98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
靶点活性	B-Raf (V600E):31 nM (cell free), Ack1:19 nM (cell free), SRMS:18 nM (cell free), C-Raf1:48 nM (cell free)
体外活性	方法：黑色素瘤细胞 A375 和 SK-Mel-28 用 Vemurafenib (0-8 μM) 处理 48 h，使用 CCK-8 assay 检测细胞活力。结果：Vemurafenib 剂量依赖性抑制 A375 和 SK-Mel-28 细胞增殖，IC50 分别为 0.8 μM 和 1.8 μM。[1] 方法：表达 BRAF V600E 的黑色素瘤细胞系 Colo829 和 LOX 用 Vemurafenib (0.05-30 μmol/L) 处理 2 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Vemurafenib 抑制了 Colo829 和 LOX 细胞中 MEK 和 ERK 的磷酸化。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Vemurafenib (12.5-75 mg/kg，suspended in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl.) 口服给药给携带黑色素瘤 LOX 的 Athymic nude 小鼠，每天两次，持续 11-13 天。结果：Vemurafenib 显著抑制肿瘤生长并诱导肿瘤消退。[2] 方法：为检测体内抗肿瘤活性，将 Vemurafenib (60 mg/kg) 口服给药给携带黑色素瘤 Colo-205 的 athymic mice 小鼠，每天两次，持续十四天。结果：Vemurafenib 有效抑制 Colo-205 异种移植小鼠模型中的肿瘤生长。[3]
激酶实验	Expression and purification of B-RAF, structure determination, and protein kinase activity measurements were carried out as previously described. To obtain co-crystals of B-RAFV600E with PLX4032, the protein solution was initially mixed with the compound dissolved in DMSO at a final compound concentration of 1 mM. This complex was co-crystallized by a sitting drop vapor diffusion experiment in which equal volumes of complex (at 10 mg/ml concentration) and reservoir solution (100mM BisTris at pH 6.0, 12.5% 2,5-hexanediol, and 12% PEG3350) were mixed and allowed to equilibrate against the reservoir at 4°C. The crystal was soaked in cryosolvent, followed by flash-freezing in liquid nitrogen. The data were collected at Beamline ALS831 with the wavelength of 1.11?. The Ramachandran plot from the refined structure shows that 94%, 5.6% and 0.4% residues are in the most favored, additional allowed and generously allowed regions, respectively. A summary of the crystallography statistics is included in Supplementary Table 3. COLO205 tumor xenograft studies (Molecular Imaging Research, Ann Arbor, MI) were carried out as previously described either using a conventional formulation (5%DMSO, 1% methylcellulose) or using the MBP formulation [1].
细胞实验	Cellular proliferation was evaluated by MTT assay. Briefly, cells were plated in 96-well microtiter plates at a density of 1,000 to 5,000 cells per well in a volume of 180 μL. For the assay, RG7204 was prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution were added to plates in duplicate. The plates were assayed for proliferation 6 days after the cells were plated according to the procedure originally described by Mosmann [2].
动物实验	All animal procedures were approved by the Ethical Commission of the Institute for Cancer Research and Treatment and by the Italian Ministry of Health. WiDr cells were injected subcutaneously into the right posterior flanks of 7-week-old immunodeficient NODSCID female mice (6 mice per group). Tumour formation was monitored twice a week, and tumour volume based on caliper measurements was calculated by the modified ellipsoidal formula: tumour volume = 1/2 length × width. When tumours reached a volume of approximately 200–250 mm^3, mice were randomly assigned to treatment with vehicle or drug(s) [3].

别名	RO5185426, RG7204, 维罗非尼, PLX4032
分子量	489.92
分子式	C23H18ClF2N3O3S
CAS No.	918504-65-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 90 mg/mL (183.7 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0411 mL	10.2057 mL	20.4115 mL	51.0287 mL
	5 mM	0.4082 mL	2.0411 mL	4.0823 mL	10.2057 mL
	10 mM	0.2041 mL	1.0206 mL	2.0411 mL	5.1029 mL
	20 mM	0.1021 mL	0.5103 mL	1.0206 mL	2.5514 mL
	50 mM	0.0408 mL	0.2041 mL	0.4082 mL	1.0206 mL
	100 mM	0.0204 mL	0.1021 mL	0.2041 mL	0.5103 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Liu C, et al. Silencing TCF4 Sensitizes Melanoma Cells to Vemurafenib Through Inhibiting GLUT3-Mediated Glycolysis. Onco Targets Ther. 2020 May 29;13:4905-4915. 2. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res. 2010 Jul 1;70(13):5518-27. 3. Zhang J, et al. EBI-907, a novel BRAF(V600E) inhibitor, has potent oral anti-tumor activity and a broad kinase selectivity profile. Cancer Biol Ther. 2016;17(2):199-207. 4. Flaherty KT, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med. 2010 Aug 26;363(9):809-19.

文献引用

1. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Vemurafenib 918504-65-1 Angiogenesis Autophagy MAPK Tyrosine Kinase/Adaptors Raf ACK Src Raf kinases PLX 4032 inhibit RG 7204 PLX-4032 Inhibitor RO-5185426 RO5185426 RG7204 RG-7204 RO 5185426 1029872-54-5 维罗非尼 PLX4032 inhibitor

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Vemurafenib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords