2. Protein Tyrosine Kinase/RTK Autophagy
  3. c-Kit Bcr-Abl PDGFR Autophagy
  4. Imatinib Mesylate

Imatinib Mesylate  (Synonyms: 甲磺酸伊马替尼; STI571 Mesylate; CGP-57148B Mesylate)

目录号: HY-50946 纯度: 99.98%
COA 产品使用指南

摩尔计算器

Imatinib Mesylate (STI571 Mesylate) 是一种酪氨酸激酶抑制剂，可抑制 c-Kit，Bcr-Abl 和 PDGFR (IC50=100 nM)。

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Imatinib Mesylate Chemical Structure

Imatinib Mesylate Chemical Structure

CAS No. : 220127-57-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550
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200 mg ￥500
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500 mg ￥900
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5 g ￥4950
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Customer Review

Other Forms of Imatinib Mesylate:

Imatinib Mesylate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 70 篇科研文献

WB
Proliferation Assay
IHC

    Imatinib Mesylate purchased from MCE. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.  [Abstract]

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in PC-9 GR NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Imatinib Mesylate purchased from MCE. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183.  [Abstract]

    Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).

    Imatinib Mesylate purchased from MCE. Usage Cited in: PLoS One. 2017 Jun 1;12(6):e0178619.  [Abstract]

    The protein expression of PDGF-A, PDGF-B, PDGF-C, and PDGF-D in hearts from mice treated with vehicle, Imatinib (IMA), ISO, IMA+ISO for one week is tested by Western blot.

    Imatinib Mesylate purchased from MCE. Usage Cited in: Med Sci Monit. 2017 Aug 6;23:3808-3816.  [Abstract]

    The kinase activity of c-Kit is enhanced in an animal model of cardiac fibrosis. The lysates of heart tissues from a mice model treated with vehicle, Imatinib (IMA), ISO, or Imatinib + ISO for one week are analyzed for phosphorylation level of p-c-Kit (Tyr719) and total protein level of c-Kit. The western blotting results from one mouse in each group and the statistical analysis of the western blotting bands are shown.

    Imatinib Mesylate purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118.  [Abstract]

    In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.

    Imatinib Mesylate purchased from MCE. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72.  [Abstract]

    Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.

    Imatinib Mesylate purchased from MCE. Usage Cited in: J Bioenerg Biomembr. 2012 Feb;44(1):155-61.  [Abstract]

    Differences in sensitivity of PDR-mutants to 3-BP, Imatinib methanesulfonate, Daunorubicin and Rhodamine 6 G. Minimal medium (YNB) with sucrose.

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    PDGFR PDGFRβ PDGFRα

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.

    IC50 & Target

    IC50: ~100 nM (c-Kit, Bcr-Abl, and PDGFR)[1]
    体外研究
    (In Vitro)

    Imatinib (STI571) Mesylate inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM[1]. Imatinib (STI571) mesylate is very effective (in vitro IC50 of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410 nM) and PDGFR (in vitro IC50, 380 nM)[2]. Imatinib (STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2[3]. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive (Ph+) acute lymphoblastic leukemia (ALL)[4].

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

    Imatinib Mesylate 相关抗体:
    体内研究
    (In Vivo)

    Animals treated with Imatinib Mesylate show a decrease of mean body weight throughout the whole study. Body weight loss is noticeable in mice from groups that receive chemotherapy and the vitamin D analog combined treatment. The body weight decrease of mice treat with both combined Imatinib mesylate and PRI-2191 is the highest (15%) on Day 22 of the experiment, but after that day, mice start to recover[4]. In a rat Ischemia/reperfusion injury (IRI) model, Imatinib mesylate attenuates lung injury by an antipermeability and antiinflammatory effect. The delivery and function of Imatinib mesylate in the lung is also confirmed in this model[5].

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

    589.71

    Formula

    C30H35N7O4S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    甲磺酸伊马替尼；格列维克
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°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 : 125 mg/mL (211.97 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)

    H2O 中的溶解度 : ≥ 50 mg/mL (84.79 mM)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.6957 mL 8.4787 mL 16.9575 mL
    5 mM 0.3391 mL 1.6957 mL 3.3915 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。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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: ≥ 2.08 mg/mL (3.53 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.53 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配置工作液。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： PBS

      Solubility: 100 mg/mL (169.57 mM); 澄清溶液; 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
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.98%

    COA (259 KB) LCMS (263 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [4]

    Tested A549 cells are placed in 96-well flat-bottom plates at a density of 5×103 cells per well 24 h before the addition of the test compounds. The cells are incubated for 96 h with two different concentrations (10 and 100 nM) of PRI-2191 and concurrently with various concentrations of Imatinib mesylate (10, 100, 1000 and 10,000 ng/mL) and other cytostatic drugs (Docetaxel (DTX) or Idarubicin (ID) : 0.1, 1, 10, 100 ng/mL; Cisplatin (CIS): 1, 10, 100, 1000 ng/mL). The sulforhodamine B (SRB) assay is performed to evaluate the cytotoxic effect. As a result, IC50 is calculated for each separate experiment in Cheburator 0.4, Dmitry Nevozhay software[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4][5]

    Mice[4]
    NOD/SCID female mice, 12-16 weeks old, body weight of 20-25 g, are used. Mice are subcutaneously (s.c.) inoculated in the right flank of the abdomen with A549 tumor cells suspension (5×106 cells in 0.2 mL of Hank’s medium per mouse, Day 0) and then are randomized into groups receiving varied combinations of vitamin D analogs and chemotherapeutics. One out of two experimental protocols is applied in the respective experiments: 1. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 75 mg/kg/day, daily for 19 days (from Days 7-25). PRI-2191 is administered s.c. or by oral gavage at a dose of 2 μg/kg/day, 3 times a week (on Days 7, 12, 14, 16, 19, 21 and 23). 2. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 50 mg/kg/day, daily for 13 days (from Days 7-19). PRI-2191 and PRI-2205 are administered s.c. at doses of 1 or 10 μg/kg/day, respectively, 3 times a week (on Days 7, 10, 12, 14, 17, 19, 21, 24 and 26). At the end of the experiments, blood is collected under anesthesia; then, the mice are sacrificed.
    Rats[5]
    Male Lewis rats weighing 270 to 320 g are used in the experiments. Imatinib mesylate (50 mg/kg) is injected intraperitoneally in the Imatinib group (n=7), and 0.5 mL of 20% DMSO without Imatinib is administered in the vehicle group (n=7). The dose of 25 mg/kg is preliminarily tested, and it produces a little improvement in lung function without statistical significance. The dose of 50 mg/kg and intraperitoneal administration are adopted based on this result and past reports. The animals undergo left thoracotomy, and the left hilum is occluded with a small metallic clamp. The occlusion is performed 20 minutes after Imatinib or vehicle administration. During clamping, the tidal volume (TV) and respiratory rate (RR) are adjusted to 8 mL/kg and 80 breaths/min, respectively. After 90 minutes of ischemia, the clamp is removed and reperfusion is maintained for 120 minutes. During reperfusion, blood flow and ventilation are restored in the bilateral lung. In the sham group (n=6), the animals are heparinized, thoracotomized, and ventilated for 210 minutes.

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

    Imatinib Mesylate 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, 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
    H2O / DMSO 1 mM 1.6957 mL 8.4787 mL 16.9575 mL 42.3937 mL
    5 mM 0.3391 mL 1.6957 mL 3.3915 mL 8.4787 mL
    10 mM 0.1696 mL 0.8479 mL 1.6957 mL 4.2394 mL
    15 mM 0.1130 mL 0.5652 mL 1.1305 mL 2.8262 mL
    20 mM 0.0848 mL 0.4239 mL 0.8479 mL 2.1197 mL
    25 mM 0.0678 mL 0.3391 mL 0.6783 mL 1.6957 mL
    30 mM 0.0565 mL 0.2826 mL 0.5652 mL 1.4131 mL
    40 mM 0.0424 mL 0.2120 mL 0.4239 mL 1.0598 mL
    50 mM 0.0339 mL 0.1696 mL 0.3391 mL 0.8479 mL
    60 mM 0.0283 mL 0.1413 mL 0.2826 mL 0.7066 mL
    80 mM 0.0212 mL 0.1060 mL 0.2120 mL 0.5299 mL
    DMSO 100 mM 0.0170 mL 0.0848 mL 0.1696 mL 0.4239 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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:

    Imatinib220127-57-1STI571CGP-57148B甲磺酸伊马替尼格列维克STI 571STI-571c-KitBcr-AblPDGFRAutophagySCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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