1. Epigenetics TGF-beta/Smad Protein Tyrosine Kinase/RTK Immunology/Inflammation Apoptosis
  2. PKC VEGFR c-Kit NO Synthase Apoptosis
  3. Midostaurin

Midostaurin  (Synonyms: 米哚妥林; PKC412; CGP 41251)

目录号: HY-10230 纯度: 99.95%
COA 产品使用指南

Midostaurin (PKC412; CGP 41251) 是一种具有口服活性的可逆多靶点蛋白激酶抑制剂。Midostaurin 抑制 PKCα/β/γSykFlk-1AktPKAc-Kitc-Fgrc-SrcFLT3PDFRβVEGFR1/2IC50 范围为 22-500 nM。Midostaurin 还上调内皮一氧化氮合酶 (eNOS) 基因表达。Midostaurin 显示出强大的抗癌作用。

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Midostaurin Chemical Structure

Midostaurin Chemical Structure

CAS No. : 120685-11-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2260
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1 mg ¥770
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5 mg ¥1800
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10 mg ¥2880
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25 mg ¥4523
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50 mg ¥7238
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200 mg   询价  

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Top Publications Citing Use of Products

    Midostaurin purchased from MCE. Usage Cited in: J Cell Mol Med. 2020 Feb;24(3):2145-2156.  [Abstract]

    Effects of Midostaurin in vivo against mice harbouring Ba/F3.FLT3(wt).CBL.Y371H-luc+ cells. Supine and Prone (High Scale), Days 12-19. Representative Images (n = 5).

    Midostaurin purchased from MCE. Usage Cited in: Haematologica. 2018 Nov;103(11):1862-1872.  [Abstract]

    Induction of tumor suppressor protein p53 in MV4-11 (A) and MOLM-13 cells (B) treated for 24 hours with the indicated amounts of NVP-HDM201 and midostaurin. Relative quantitation of CDKN1A mRNA (C) and MCL-1 mRNA (D) in AML cells treated for 24 hours with PKC412 and NVP-HDM201 alone or in combination.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1][2]. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects[3].

    IC50 & Target[2]

    cPKC-α

    22 nM (IC50)

    eNOS

     

    cPKC-γ

    24 nM (IC50)

    cPKC-β1

    30 nM (IC50)

    cPKC-β2

    31 nM (IC50)

    nPKC-δ

    33 nM (IC50)

    nPKC-η

    160 nM (IC50)

    nPKC-ε

    1250 nM (IC50)

    aPKC-ζ

    465000 nM (IC50)

    PPK

    38 nM (IC50)

    KDR

    86 nM (IC50)

    c-Syk

    95 nM (IC50)

    cdk1/cycB

    570 nM (IC50)

    Protein kinase A

    570 nM (IC50)

    c-Fgr

    790 nM (IC50)

    c-Src

    800 nM (IC50)

    Flt-1

    912 nM (IC50)

    EGF-R

    1100 nM (IC50)

    Myosin-light chain kinase

    1900 nM (IC50)

    Flk-1

    3900 nM (IC50)

    c-Lyn

    4300 nM (IC50)

    P70S6 kinase

    5000 nM (IC50)

    CSK

    8000 nM (IC50)

    体外研究
    (In Vitro)

    Midostaurin (PKC412) 在体外对各种肿瘤和正常细胞系表现出广泛的抗增殖活性,并且能够在体外逆转 Pgp 介导的肿瘤细胞多药耐药性。细胞暴露于 Midostaurin (PKC412) 会导致细胞周期的 G2/M 期剂量依赖性增加,同时多倍体增加、细胞凋亡和电离辐射敏感性增强[1]
    Midostaurin (PKC412) 显著抑制 KIT-、Lyn-和 STAT5 活性,但不抑制 HMC-1 细胞和原发性肿瘤肥大细胞中的 Btk[3]
    Midostaurin (PKC412) 抑制造血 Ba/F3 细胞中的 EN 融合酪氨酸激酶。Midostaurin (PKC412) 以剂量依赖性方式显著抑制 M0-91 和 IMS-M2 细胞中的 EN 磷酸化[4]

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

    体内研究
    (In Vivo)

    Midostaurin (PKC412) 强烈抑制小鼠模型中的视网膜新生血管形成以及激光诱导的脉络膜新生血管形成[1]
    Midostaurin (PKC412) (25 mg/kg,腹腔注射) 保护 K18 Arg90Cys 过表达转基因小鼠的小鼠肝脏免受 Fas 诱导的细胞凋亡[5]

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

    Clinical Trial
    分子量

    570.64

    Formula

    C35H30N4O4

    CAS 号
    性状

    固体

    颜色

    White to yellow

    中文名称

    米哚妥林

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (87.62 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 1.7524 mL 8.7621 mL 17.5242 mL
    5 mM 0.3505 mL 1.7524 mL 3.5048 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

    • 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.38 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (4.38 mM); 澄清溶液

      此方案可获得 ≥ 2.5 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.95%

    参考文献
    Cell Assay
    [3]

    Proliferation is determined by trypan blue dye exclusion test. Cells in suspension are seeded in six-well plates at a density of 1×105 cells/mL in the presence of different concentrations of PKC412 for 3 days. In control wells, DMSO instead of Midostaurin (PKC412) is added. After the treatment, 10 μL of the cell suspension is mixed with 10 μL of 0.4% trypan blue, and alive cells are counted manually using a hemacytometer. Results are calculated as the percentage of the values measured when cells are grown in the absence of the reagent. All experiments are performed in triplicate[3].

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

    Animal Administration
    [4]

    K8-deficient, K18-deficient, and human K18 R90C-overexpressing mice with age of 6-8 weeks are used in the assay. Age and sex matched mice are treated with Midostaurin (25 mg/kg), daily for 4 d or with an equal volume of DMSO as vehicle (both administered intraperitoneally). On day 5 post-treatment, apoptosis is induced by intraperitoneal injection of Fas ligand (Fas-L) (0.15 μg/g body weight). Mice are fasted overnight before Fas Ab injection, and 18 mice are used per DMSO or Midostaurin (PKC412) group for the Fas-treated mice while 6 mice are used per DMSO or Midostaurin (PKC412) group for the control non-Fas-treated mice. Mice are sacrificed by CO2 inhalation 6 h after Fas Ab injection. Blood is collected by intracardiac puncture, and livers are harvested for hematoxylin and eosin (HE) staining (after fixation in 10% formalin) or frozen in optimum cutting temperature compound for immunofluorescence staining[4].

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

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7524 mL 8.7621 mL 17.5242 mL 43.8105 mL
    5 mM 0.3505 mL 1.7524 mL 3.5048 mL 8.7621 mL
    10 mM 0.1752 mL 0.8762 mL 1.7524 mL 4.3810 mL
    15 mM 0.1168 mL 0.5841 mL 1.1683 mL 2.9207 mL
    20 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1905 mL
    25 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7524 mL
    30 mM 0.0584 mL 0.2921 mL 0.5841 mL 1.4603 mL
    40 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
    50 mM 0.0350 mL 0.1752 mL 0.3505 mL 0.8762 mL
    60 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
    80 mM 0.0219 mL 0.1095 mL 0.2191 mL 0.5476 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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    目录号:
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