Home > MEK & > Trametinib

Trametinib

曲美替尼,GSK1120212,JTP-74057

Trametinib (GSK1120212)是一种高特异性的，有效的MEK1/2抑制剂，IC50为0.92 nM/1.8 nM，对c-Raf， B-Raf， ERK1/2没有抑制活性。

目录号
EY0677
EY0677
EY0677
纯度
99.36%
99.36%
99.36%
规格
5 mg
10 mg
50 mg
原价
190
270
680
售价
190
270
680
库存
现货
现货
现货
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  • 生物活性

    Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% Propylene glycol

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    1 mg/kg/day 口服

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Yamaguchi T, et al. Int J Oncol, 2011, 39(1), 23-31.

    分子式
    C26H23FIN5O4    		 分子量
    615.39    		 CAS号
    871700-17-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >20 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01941927 Melanoma Drug: Trametinib (GSK1120212)|Drug: GSK2141795 Adil Daud|National Comprehensive Cancer Network|University of California, San Francisco Phase 2 2013-09-01 2015-02-17
    NCT03087448 Non-small Cell Lung Cancer Drug: Ceritinib|Drug: Trametinib University of California, San Francisco|Novartis Pharmaceuticals|University of California, Davis|University of California, Los Angeles|University of California, San Diego|University of California, Irvine Phase 1|Phase 2 2017-03-01 2017-03-16
    NCT01958112 Cervical Cancer Drug: GSK1120212 (trametinib)|Drug: GSK2141795 Dana-Farber Cancer Institute|Novartis|National Comprehensive Cancer Network Phase 2 2013-10-01 2016-08-10
    NCT02939846 Cancer Drug: Trametinib GlaxoSmithKline Phase 1 2017-05-01 2017-01-25
    NCT01553851 Neoplasms, Oral|Mouth Neoplasms Drug: GSK1120212 Washington University School of Medicine|National Comprehensive Cancer Network Phase 2 2013-02-01 2016-10-31
    NCT02070549 Advanced Solid Neoplasm|Hepatic Complication|Metastatic Malignant Neoplasm in the Liver|Metastatic Solid Neoplasm|Unresectable Solid Neoplasm Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Trametinib National Cancer Institute (NCI) Phase 1 2014-02-01 2017-01-31
    NCT01740648 Recurrent Rectal Cancer|Stage IIA Rectal Cancer|Stage IIB Rectal Cancer|Stage IIC Rectal Cancer|Stage IIIA Rectal Cancer|Stage IIIB Rectal Cancer|Stage IIIC Rectal Cancer Drug: trametinib|Drug: fluorouracil|Radiation: radiation therapy Evan Wuthrick|National Comprehensive Cancer Network|Novartis Pharmaceuticals|Ohio State University Comprehensive Cancer Center Phase 1 2012-11-01 2016-11-14
    NCT01972347 Melanoma Drug: Dabrafenib|Drug: Trametinib Melanoma Institute Australia Phase 2 2014-10-01 2017-03-21
    NCT02231775 Melanoma Drug: Dabrafenib|Drug: Trametinib|Procedure: Surgery M.D. Anderson Cancer Center|Novartis Pharmaceuticals Phase 2 2014-10-01 2017-02-10
    NCT02140840 Multiple Myeloma Drug: Trametinib University of Arkansas Phase 2 2015-03-01 2016-04-06
    NCT03085056 Anaplastic Thyroid Cancer Drug: Trametinib|Drug: Paclitaxel Memorial Sloan Kettering Cancer Center|Novartis 2017-03-15 2017-03-21
    NCT02428270 Pancreatic Cancer|Adenocarcinoma Drug: GSK2256098|Drug: Trametinib University Health Network, Toronto|GlaxoSmithKline Phase 2 2016-04-01 2016-10-05
    NCT01964924 Estrogen Receptor Negative|HER2/Neu Negative|Invasive Breast Carcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma Drug: Akt Inhibitor GSK2141795|Other: Laboratory Biomarker Analysis|Drug: Trametinib National Cancer Institute (NCI)|GlaxoSmithKline Phase 2 2013-10-01 2017-03-03
    NCT01726738 Stage III Melanoma|Stage IV Melanoma|Unresectable Melanoma|BRAF Mutant Melanoma Drug: BRAF inhibitor dabrafenib and MEK inhibitor trametinib UNC Lineberger Comprehensive Cancer Center|GlaxoSmithKline Phase 2 2012-10-01 2017-03-02
    NCT02447939 Melanoma Drug: Dabrafenib|Drug: Trametinib GlaxoSmithKline Phase 1 2017-05-01 2017-01-25
    NCT03076164 Lung Adenocarcinoma|Lung Cancer|Lung Cancer Metastatic|Lung Cancer Stage IV|Recurrent Lung Adenocarcinoma|Recurrent Lung Cancer Drug: Trametinib|Drug: Erlotinib Memorial Sloan Kettering Cancer Center|GlaxoSmithKline Phase 1|Phase 2 2017-03-01 2017-03-09
    NCT02300935 Melanoma Drug: trametinib|Drug: nab-paclitaxel SCRI Development Innovations, LLC|Celgene Corporation|GlaxoSmithKline Phase 1 2016-01-01 2016-01-14
    NCT02416232 Melanoma Drug: Trametinib|Drug: Dabrafenib GlaxoSmithKline Phase 3 2015-03-01 2017-02-23
    NCT02292173 Hepatocellular Cancer|Liver Cancer Drug: Trametinib|Drug: Sorafenib H. Lee Moffitt Cancer Center and Research Institute Phase 1 2014-12-19 2017-01-23
    NCT02015117 Metastatic Malignant Neoplasm in the Brain Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Procedure: Therapeutic Conventional Surgery|Drug: Trametinib|Radiation: Whole-Brain Radiotherapy National Cancer Institute (NCI) Phase 1 2014-01-01 2016-12-14
    NCT02672358 Non-Small-Cell Lung Cancer Drug: Dabrafenib|Drug: Trametinib Novartis Pharmaceuticals|Novartis Phase 2 2017-10-01 2017-01-03

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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