1. Protein Tyrosine Kinase/RTK Autophagy MAPK/ERK Pathway
  2. VEGFR Autophagy PDGFR Raf RET c-Kit FGFR Tie
  3. Regorafenib

Regorafenib  (Synonyms: 瑞戈非尼; BAY 73-4506)

目录号: HY-10331 纯度: 99.93%
COA 产品使用指南

Regorafenib (BAY 73-4506) 是一种口服有效的多靶点受体酪氨酸激酶 (tyrosine kinase) 抑制剂,抑制 VEGFR1/2/3PDGFRβKitRETRaf-1IC50 分别为 13/4.2/46,22,7,1.5 和 2.5 nM。Regorafenib 显示出非常强的抗肿瘤和抗血管生成活性。

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Regorafenib Chemical Structure

Regorafenib Chemical Structure

CAS No. : 755037-03-7

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10 mM * 1 mL in DMSO ¥500
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5 mg ¥237
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10 mg ¥380
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50 mg ¥950
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500 mg ¥4500
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 45 篇科研文献

WB

    Regorafenib purchased from MCE. Usage Cited in: Neoplasia. 2023 Mar 18;39:100897.  [Abstract]

    Regorafenib (0-40 µM; 36 h) markedly increases the expression of cleaved caspase-3, while decreases the expression of anti-apoptotic protein Bcl-2, in both H1299 and PC-9 cells.

    Regorafenib purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915.  [Abstract]

    Effects on the expression of phosphorylated extracellular signal-related kinase (p-ERK), ERK, thymidylate synthase (TS), and markers of cell death in SW620, HCT 116, and HT-29 cells using various Regorafenib treatment schedules.

    Regorafenib purchased from MCE. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983.  [Abstract]

    The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

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    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity[1].

    IC50 & Target[1]

    Raf-1

    2.5 nM (IC50)

    Tie2

    311 ± 46 nM (IC50)

    VEGFR2

    4.2 nM (IC50)

    VEGFR1

    13 nM (IC50)

    BRafV600E

    19 nM (IC50)

    PDGFRβ

    22 nM (IC50)

    Braf

    28 nM (IC50)

    VEGFR3

    46 nM (IC50)

    体外研究
    (In Vitro)

    Regorafenib (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells[1].
    Regorafenib (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2[1].
    Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[3].

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

    Cell Proliferation Assay[1]

    Cell Line: GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells
    Concentration: 10 μM and 5 nM
    Incubation Time: 96 h
    Result: Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.

    Western Blot Analysis[1]

    Cell Line: NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells
    Concentration: 0, 10, 30, 100, 300, 1000, 3000 nM
    Incubation Time: 30 min
    Result: Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC50 values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2.
    体内研究
    (In Vivo)

    Regorafenib (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model[1].
    Regorafenib (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model[1].

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

    Animal Model: Rat GS9L glioblastoma xenograft[1]
    Dosage: 10 mg/kg
    Administration: Orally, single dose or daily for 4 days
    Result: Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
    Animal Model: Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors[1]
    Dosage: 0, 3, 10, 30, 100 mg/kg
    Administration: Orally, qd × 9
    Result: Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation.
    Clinical Trial
    分子量

    482.82

    Formula

    C21H15ClF4N4O3

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    瑞戈非尼;瑞格非尼;瑞格菲尼

    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (258.90 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 2.0712 mL 10.3558 mL 20.7117 mL
    5 mM 0.4142 mL 2.0712 mL 4.1423 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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

    In Vivo:

    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    90% Corn Oil

      Solubility: ≥ 7.5 mg/mL (15.53 mM); 澄清溶液

      此方案可获得 ≥ 7.5 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。

      1 mL 工作液为例,取 100 μL 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 方案 二

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.75 mg/mL (5.70 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

    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: 99.93%

    参考文献

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0712 mL 10.3558 mL 20.7117 mL 51.7791 mL
    5 mM 0.4142 mL 2.0712 mL 4.1423 mL 10.3558 mL
    10 mM 0.2071 mL 1.0356 mL 2.0712 mL 5.1779 mL
    15 mM 0.1381 mL 0.6904 mL 1.3808 mL 3.4519 mL
    20 mM 0.1036 mL 0.5178 mL 1.0356 mL 2.5890 mL
    25 mM 0.0828 mL 0.4142 mL 0.8285 mL 2.0712 mL
    30 mM 0.0690 mL 0.3452 mL 0.6904 mL 1.7260 mL
    40 mM 0.0518 mL 0.2589 mL 0.5178 mL 1.2945 mL
    50 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0356 mL
    60 mM 0.0345 mL 0.1726 mL 0.3452 mL 0.8630 mL
    80 mM 0.0259 mL 0.1294 mL 0.2589 mL 0.6472 mL
    100 mM 0.0207 mL 0.1036 mL 0.2071 mL 0.5178 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.

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    产品名称:
    Regorafenib
    目录号:
    HY-10331
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