2. MAPK/ERK Pathway Autophagy Apoptosis
  3. MEK Autophagy Apoptosis
  4. Trametinib

Trametinib  (Synonyms: 曲美替尼; GSK1120212; JTP-74057)

目录号: HY-10999 纯度: 99.96%
COA 产品使用指南

摩尔计算器

Trametinib (GSK1120212; JTP-74057) 是口服有效的 MEK 抑制剂，抑制 MEK1 和 MEK2 的 IC50 分别为 2 nM。Trametinib 可以激活自噬 (autophagy)，诱导凋亡 (apoptosis)。

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Trametinib Chemical Structure

Trametinib Chemical Structure

CAS No. : 871700-17-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥385
In-stock
5 mg ￥218
In-stock
10 mg ￥350
In-stock
50 mg ￥780
In-stock
100 mg ￥1250
In-stock
500 mg ￥3300
In-stock
1 g   询价  
5 g   询价  

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Customer Review

Other Forms of Trametinib:

Trametinib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 186 篇科研文献

WB

    Trametinib 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 PLX4032 (1 μM), GSK2118436A (100 nM), or Trametinib (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

    Trametinib purchased from MCE. Usage Cited in: Oncogenesis. 2019 Nov 4;8(11):65.  [Abstract]

    Western blot analysis of p-ERK and ERK protein levels in cell lysates of H1975 treated with AMPC, Trametinib for 24 h. The levels of the total ERK was used as an input control.

    Trametinib purchased from MCE. Usage Cited in: J Cell Sci. 2019 May 31;132(11):jcs224071.  [Abstract]

    Western blots of phosphorylated active ERK1/2 (pERK) and total ERK1/2 (ERK) for MDA MB 231 Sel2 and MDA MB 435 Sel1 populations following treatment with DMSO vehicle, 0.5 μM Trametinib or 10 μM U0126 for 18 h.

    Trametinib purchased from MCE. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.  [Abstract]

    MEK inhibitor Trametinib (GSK1120212) achieves target inhibition at 3mg/kg.

    Trametinib purchased from MCE. Usage Cited in: Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.  [Abstract]

    Western blot analysis of selected MAPK and AKT/mTOR pathway components in Trametinib- and CCI-779-treated cells.

    Trametinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Sep 5;37(1):218.  [Abstract]

    WB for ERRα, IDH3A, c-Myc and Cyclin D1 in the HCT116 and SW480 cells treated with the indicated concentrations of Trametinib (0-100 nM) or DMSO for 48 h.

    Trametinib purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Oct 9;115(41):E9570-E9579.  [Abstract]

    presentative Western blots used to measure the efficiencies of kinase inhibitors in reducing ERK1/2 phosphorylation in control, ERK1/2 inhibitor (FR180204 and SCH772984; 10 μM)-treated or MEK1/2 inhibitor (GSK1120212; 10 μM)-treated ARPE-19 and H1299 cells.

    Trametinib purchased from MCE. Usage Cited in: Eur J Cancer. 2018 Aug;99:37-48.  [Abstract]

    Western blot detection of cleaved PARP in H358, SW480 and HCT-116 cell lines treated with BMS-354825 (100 nM), Trametinib (400 nM) or combination for 48 h. DMSO is used as the treatment control.

    Trametinib purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Jan 8;495(2):1846-1850.  [Abstract]

    Western blot analysis of phosphorylated ERK2, and ERK2 in microvesicle-depleted fraction (15 μg of protein) derived from viruses obtained from 10 nM Trametinib-treated CEM/LAV-1 cells.

    Trametinib purchased from MCE. Usage Cited in: Patent. US20180161326A1.

    Trametinib (100 nM) and PLX4032 (10 μM) in combination have little effect on PARP-1 cleavage in A375 and UACC-62 cells, but significant PARP-1 cleavage and reduction in procaspase-3 level are observed via Western blot with the addition of PAC-1 (12 μM).

    Trametinib purchased from MCE. Usage Cited in: Patent. US20180169102A1.

    The presence or absence of the pERK protein are measured through western blotting using the brain hemispheres of trametinib-administered 5×FAD mice.

    Trametinib purchased from MCE. Usage Cited in: Sci Rep. 2017 Mar 28;7:45332.  [Abstract]

    Trametinib, a MEK1/2 inhibitor, strongly inhibits growth and partially reverses GW786034 resistance of GW786034-resistant clones.Trametinib-induced inhibition of phosphorylation of ERK1/2 in SS clones is assessed by Western blot analysis with anti-ERK1/2 and anti-phospho-ERK1/2 antibodies. SS clones are pre-treated using 10 nMtrametinib for 2 hours.

    Trametinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846.  [Abstract]

    MEK inhibition results in reduced ERK phosphorylation.A. Western blot analysis of SEM and KOPN8 exposed to 500 nM of MEK inhibitor or vehicle control (DMSO) for 6, 24 and 48 hours. Both cell lines almost completely lose ERK phosphorylation (p-ERK), while total ERK (t-ERK) levels remain unaffected. B. Analysis of MEK phosphorylation (p-MEK) suggests exposure to MEK162 and Selumetinib results in enhanced MEK phosphorylation in both cell lines, whereas total MEK (t-MEK) levels remain constant.

    Trametinib purchased from MCE. Usage Cited in: Stem Cell Reports. 2016 Jan 12;6(1):74-84.  [Abstract]

    Western blot of SKPs treated with varying concentrations of Trametinib (MEKi) or DMSO (Control) for 30 min, probed for pERK1/2 and reprobed for total ERK1/2.

    Trametinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Aug;15(8):1859-69.  [Abstract]

    Addition of PAC-1 to the combination of PLX4032+Trametinib powerfully synergizes to induce apoptotic death and caspase activity in A375 and UACC-62 cells. Trametinib (100 nM) and PLX4032 (10 μM) in combination have little effect on PARP-1 cleavage in A375 and UACC-62 cells, but significant PARP-1 cleavage and reduction in procaspase-3 level are observed via Western blot with the addition of PAC-1 (12 μM).

    Trametinib purchased from MCE. Usage Cited in: J Cell Biochem. 2016 Jun;117(6):1340-51.  [Abstract]

    HeLa S3 cells that are arrested at the G2/M border by RO-3306 treatment are washed free of RO-3306 and incubated with 10 μM GSK1120212.

    Trametinib purchased from MCE. Usage Cited in: Cancer Discov. 2015 Sep;5(9):960-71.  [Abstract]

    The MEK inhibitor Trametinib effectively inhibits ERK phosphorylation at 30 nM in several EGFR mutant cell lines but has little effect on cell viability.

    查看 MEK 亚型特异性产品:

    查看所有亚型
    MEK1 MEK2 MEK5 MEK

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].

    IC50 & Target[1]

    MEK1

    2 nM (IC50)

    MEK2

    2 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.46 μM
    Compound: 1
    Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    		[PMID: 32305784]
    DLD-1 IC50
    1.34 μM
    Compound: 39
    Anticancer activity against human DLD-1 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay
    Anticancer activity against human DLD-1 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay
    		[PMID: 33445154]
    HCT-116 IC50
    0.019 μM
    Compound: 1
    Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    		[PMID: 32305784]
    HCT-116 IC50
    1.16 μM
    Compound: 39
    Anticancer activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay
    Anticancer activity against human HCT-116 cells assessed as reduction in cell viability incubated for 24 hrs by Cell Titer-Glo assay
    		[PMID: 33445154]
    HL-60 IC50
    0.003 μM
    Compound: 1
    Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    		[PMID: 32305784]
    MDA-MB-231 IC50
    0.018 μM
    Compound: 1
    Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
    		[PMID: 32305784]
    MDA-MB-231 GI50
    25 nM
    Compound: trametinib
    Growth inhibition of human MDA-MB-231 cells after 3 days by DAPI staining
    Growth inhibition of human MDA-MB-231 cells after 3 days by DAPI staining
    		10.1039/C3MD00290J
    体外研究
    (In Vitro)

    Trametinib (GSK1120212；JTP-74057) (0.1-100 nM) 阻断外周血单核细胞 (PBMC) 中肿瘤坏死因子-α 和白细胞介素 6 的产生。Trametinib (JTP-74057) 抑制 10 种人结直肠癌细胞系中的 9 种的生长，并且它们在药物处理后显示细胞周期停滞在 G1 期[1]。
    GSK2118436 和 Trametinib (GSK1120212) 的组合有效抑制细胞生长，降低 ERK 磷酸化，减少细胞周期蛋白 D1 蛋白，并增加耐药克隆中的 p27 (kip1) 蛋白[2]。

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

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

    佐剂性关节炎 (AIA) 和 II 型胶原性关节炎 (CIA) 的发展几乎完全被 0.1 mg/kg 的 Trametinib (GSK1120212;JTP-74057) 或 10mg /kg HWA486 抑制[1]。
    Trametinib (0.3 mg/kg，1 mg/kg，po) 在裸鼠异种移植模型中有效抑制 HT-29 异种移植物的生长[2]。

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

    615.39

    Formula

    C26H23FIN5O4
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    曲美替尼
    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 25 mg/mL (40.62 mM; 超声助溶 (<60°C); 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 1.6250 mL 8.1249 mL 16.2499 mL
    5 mM 0.3250 mL 1.6250 mL 3.2500 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。-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

    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: ≥ 2.5 mg/mL (4.06 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。

      以 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 (4.06 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。

      以 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。

    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： 0.5% HPMC/1% Tween-80 in Saline water

      Solubility: 6.67 mg/mL (10.84 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: 99.96%

    COA (295 KB) RP-HPLC (242 KB) 元素分析报告 (217 KB)

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

    The nonphosphorylated myelin basic protein (MBP) is coated onto an ELISA plate, and the active form of B-Raf/c-Raf is mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 µM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of Trametinib (JTP-74057). The phosphorylation of MBP is detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases are tested at 10 µM ATP[2].

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

    Cells are treated with various concentrations of Trametinib (JTP-74057) in 100 mm dishes for 3 or 4 days. Both floating and adherent cells are collected and fixed with 70% ethanol. After washing with PBS, the cells are suspended in 100 µL/mL RNase and 25 µL/mL Propidium iodide (PI) and incubated at 37°C for 30 min in the dark. The DNA content of each single cell is determined using the flow cytometer Cytomics FC500 or Guava EasyCyte plus[2].

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

    Mice[2]
    Female BALB/c-nu/nu mice are used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) are inoculated subcutaneously into the right flank of the mice at 5×106 cells/100 µL/site or 1×106 cells/100 µL/site, respectively. The acetic acid-solvated form of Trametinib (JTP-74057, 0.3 mg/kg, 1 mg/kg) is dissolved in 10% Cremophor EL-10% PEG400 and is administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm3. The tumor length [L(mm)] and width [W(mm)] are measured using a microgauge twice a week after commencement of dosing, and the tumor volume is calculated using the following formula: tumor volume (mm3)=L×W×W/2.

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

    Trametinib 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。-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 1.6250 mL 8.1249 mL 16.2499 mL 40.6246 mL
    5 mM 0.3250 mL 1.6250 mL 3.2500 mL 8.1249 mL
    10 mM 0.1625 mL 0.8125 mL 1.6250 mL 4.0625 mL
    15 mM 0.1083 mL 0.5417 mL 1.0833 mL 2.7083 mL
    20 mM 0.0812 mL 0.4062 mL 0.8125 mL 2.0312 mL
    25 mM 0.0650 mL 0.3250 mL 0.6500 mL 1.6250 mL
    30 mM 0.0542 mL 0.2708 mL 0.5417 mL 1.3542 mL
    40 mM 0.0406 mL 0.2031 mL 0.4062 mL 1.0156 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:

    Trametinib871700-17-3GSK1120212 JTP-74057曲美替尼GSK 1120212GSK-1120212JTP74057JTP 74057JTP-74057MEKAutophagyApoptosisMitogen-activated protein kinase kinaseMAPKKMAP2KAdjuvant-inducedarthritisAIAtypeIIcollageninducedCIAorallyInhibitorinhibitorinhibit

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