2. MAPK/ERK Pathway Autophagy
  3. Raf Autophagy
  4. Vemurafenib

Vemurafenib  (Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426)

目录号: HY-12057 纯度: 99.85%
COA 产品使用指南

摩尔计算器

Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的，有效的 B-RAF 选择性抑制剂，能够抑制 RAFV600E 和 c-RAF-1 的活性，IC50 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。

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Vemurafenib Chemical Structure

Vemurafenib Chemical Structure

CAS No. : 918504-65-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥567
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5 mg ￥321
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10 mg ￥515
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50 mg ￥1450
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100 mg ￥2320
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Customer Review

Other Forms of Vemurafenib:

Vemurafenib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 75 篇科研文献

WB

    Vemurafenib purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jan;39:194-206.  [Abstract]

    Western analysis of related proteins expression with or without the treatment of vemurafenib and other treatments. Left: M6 are transfected with PLAUR siRNA and negative control siRNA and incubated for 48 h in presence of 1 μM vemurafenib. Right: A375 are transfected either with Mock or uPAR overexpressing plasmid pQ2-uPAR. After 24 h are seeded at the same density (800 cells/ml) and cultured in the presence of vemurafenib at indicated concentrations for 10 days.

    Vemurafenib purchased from MCE. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.  [Abstract]

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with Vemurafenib (1 μM), GSK2118436A (100 nM), or GSK1120212 (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

    Vemurafenib purchased from MCE. Usage Cited in: Oncogene. 2018 Oct;37(43):5719-5734.  [Abstract]

    BRAF mutants with in-frame β3-αC loop deletions exhibit a robust but differential inhibitor resistance. Stable fibroblast cells that express individual BRAF mutants with in-frame β3-αC loop deletions are treated with Vemurafenib for 4 h, and p-ERK1/2 is probed by immunoblot and quantified.

    Vemurafenib purchased from MCE. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950.  [Abstract]

    Western analysis of protein expression in cells treatmented with or without PLX4032 or RAD001.

    Vemurafenib purchased from MCE. Usage Cited in: Mol Syst Biol. 2017 Jan; 13(1): 905.  [Abstract]

    Western blotting for NGFR-inducible COLO858 cells, NGFRHigh A375 and WM115 cells, and NGFRLow MACSF and MZ7MEL cells, treated for 48 h with 0.2 or 1 μM Vmurafenib or DMSO.

    Vemurafenib purchased from MCE. Usage Cited in: Cancer Lett. 2017 Nov 1;408:43-54.  [Abstract]

    Western blot analysis of p-ERK, ERK, p-AKT and ERK after 24 h of treatment with Vemurafenib. Levels of p-ERK and p-AKT are quantified by densitometric analysis and a corresponding histogram is constructed as relative to ERK or AKT and α-tubulin. Representative Western blot panels on the left.

    Vemurafenib purchased from MCE. Usage Cited in: J Mol Med (Berl). 2017 Jan;95(1):97-108.  [Abstract]

    Immunoblotting of phosphorylated and total EGFR,AKT, and ERK1/2 in A375-M6 clones treated or not with 0.5 μMvemurafenib for 24 h. 50 μL/ well loaded. Tubulin detected as loading control. Quantification (right) of phosphorylated protein on total protein, normalized on housekeeper (Tubulin).

    Vemurafenib purchased from MCE. Usage Cited in: Clin Cancer Res. 2013 Feb 1;19(3):598-609.  [Abstract]

    MEKi decreases PD-L1 expression in BRAFi-resistant cells. A, immunoblot analyses of the activities of ERK1/2 and c-Jun in the K028, M34, and K029 parental lines treated with U0126 (U; 20 μM), PLX4032 (PLX; 10 μM), or the combination of U0126 (20 μM) and PLX4032 (10 μM) for 30 minutes. Cells are treated with DMSO (D) as controls. B, immunoblot example showing decrease in PD-L1 expression in parental M34 cells treated with U0126, PLX4032, or the combination.

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    BRaf c-Raf Raf

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

    IC50 & Target[1]

    B-RafV600E

    31 nM (IC50)

    c-Raf-1

    48 nM (IC50)

    体外研究
    (In Vitro)

    Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Vemurafenib 相关抗体:
    体内研究
    (In Vivo)

    Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    489.92

    Formula

    C23H18ClF2N3O3S
    CAS 号
    性状

    固体

    颜色

    White to gray

    中文名称

    维罗非尼；维罗菲尼；威罗菲尼；唯罗非尼
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (102.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0411 mL 10.2057 mL 20.4115 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    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分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

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

      Solubility: ≥ 2.08 mg/mL (4.25 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.25 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 1.5% CMC-Na/saline water

      Solubility: 3.33 mg/mL (6.80 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.85%

    COA (287 KB) HNMR (280 KB) RP-HPLC (198 KB) LCMS (94 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Briefly, cells are 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, Vemurafenib (RG7204) is 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 are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated according to the procedure.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Athymic nude mice, are with ages 13 to 14 weeks, and weighing approximately 23 to 25 g. For the LOX xenografts, 2×106 cells in 0.2 mL of PBS are injected s.c. into the right lateral flank. Vemurafenib (RG7204), formulated as MBP, is suspended at the desired concentration as needed for each dose group in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl. NSC 362856 is of 250-mg capsules. Capsules are opened and combined into one bulk supply. To prepare the stock dosing material, NSC 362856 is first dissolved in 100% DMSO followed by dilution with saline to form a final milky white suspension in 10% DMSO/90% saline (pH 3.4).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Vemurafenib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 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
    15 mM 0.1361 mL 0.6804 mL 1.3608 mL 3.4019 mL
    20 mM 0.1021 mL 0.5103 mL 1.0206 mL 2.5514 mL
    25 mM 0.0816 mL 0.4082 mL 0.8165 mL 2.0411 mL
    30 mM 0.0680 mL 0.3402 mL 0.6804 mL 1.7010 mL
    40 mM 0.0510 mL 0.2551 mL 0.5103 mL 1.2757 mL
    50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0206 mL
    60 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8505 mL
    80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6379 mL
    100 mM 0.0204 mL 0.1021 mL 0.2041 mL 0.5103 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vemurafenib918504-65-1PLX4032 RG7204 RO5185426维罗非尼维罗菲尼威罗菲尼唯罗非尼PLX 4032PLX-4032RG7204RG 7204RG-7204RO5185426RO 5185426RO-5185426RafAutophagyRaf kinasesInhibitorinhibitorinhibit

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