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

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

目錄號(hào): HY-10999 純度: 99.96%
COA 產(chǎn)品使用指南 技術(shù)支持

Trametinib (GSK1120212; JTP-74057) 是口服有效的 MEK 抑制劑，抑制 MEK1 和 MEK2 的 IC50 分別為 2 nM。Trametinib 可以激活自噬 (autophagy)，誘導(dǎo)凋亡 (apoptosis)。

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Trametinib Chemical Structure

Trametinib Chemical Structure

CAS No. : 871700-17-3

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規(guī)格 價(jià)格 是否有貨 數(shù)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   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Trametinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 206 篇科研文獻(xiàn)

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 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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)

    細(xì)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
    體外研究
    (In Vitro)

    Trametinib (GSK1120212；JTP-74057) (0.1-100 nM) 阻斷外周血單核細(xì)胞 (PBMC) 中腫瘤壞死因子-α 和白細(xì)胞介素 6 的產(chǎn)生。Trametinib (JTP-74057) 抑制 10 種人結(jié)直腸癌細(xì)胞系中的 9 種的生長(zhǎng)，并且它們?cè)谒幬锾幚砗箫@示細(xì)胞周期停滯在 G1 期[1]。
    GSK2118436 和 Trametinib (GSK1120212) 的組合有效抑制細(xì)胞生長(zhǎng)，降低 ERK 磷酸化，減少細(xì)胞周期蛋白 D1 蛋白，并增加耐藥克隆中的 p27 (kip1) 蛋白[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    佐劑性關(guān)節(jié)炎 (AIA) 和 II 型膠原性關(guān)節(jié)炎 (CIA) 的發(fā)展幾乎完全被 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) 在裸鼠異種移植模型中有效抑制 HT-29 異種移植物的生長(zhǎng)[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 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    曲美替尼
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 25 mg/mL (40.62 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.06 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.06 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% HPMC/1% Tween-80 in Saline water

      Solubility: 6.67 mg/mL (10.84 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.96%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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.

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