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/ MEK / Trametinib

曲美替尼 /Trametinib 99%+

货号：A188937 同义名： JTP-74057;GSK1120212 Ambeed 开学季，买赠积分，赢豪礼

Trametinib (GSK1120212；JTP-74057) 是一种口服活性的 MEK 抑制剂，抑制 MEK1 和 MEK2 的 IC50 值约为 2 nM。Trametinib 激活自噬并诱导细胞凋亡。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Trametinib 化学结构 CAS号：871700-17-3
Trametinib 化学结构
CAS号：871700-17-3
Trametinib 3D分子结构
CAS号：871700-17-3
Trametinib 化学结构 CAS号：871700-17-3
Trametinib 3D分子结构 CAS号：871700-17-3
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Trametinib 纯度/质量文件 产品仅供科研

货号：A188937 标准纯度： 99%+
批次查询： 批次纯度:

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产品名称 MEK ↓ MEK1 ↓ MEK1/2 ↓ MEK2 ↓ MEK5 ↓ 其他靶点 纯度
Honokiol ✔ 98%
Mirdametinib ++++

MEK, IC50: 0.33 nM

 		99%+
Binimetinib +++

MEK, IC50: 12 nM

 		99%+
BI-847325 ++

MEK1, IC50: 25 nM

 		+++

MEK2, IC50: 4 nM

 		99%+
U0126-EtOH +

MEK1, IC50: 0.07 μM

 		++

MEK2, IC50: 0.06 μM

 		98%
GDC-0623 ++++

MEK1, IC50: 0.13 nM

 		99%+
TAK-733 ++++

MEK1, IC50: 3.2 nM

 		99%+
Trametinib ++++

MEK1, IC50: 0.92 nM

 		++++

MEK2, IC50: 1.8 nM

 		99%+
Selumetinib +++

MEK1, IC50: 14 nM

MEK1, Kd: 99 nM

 		+

MEK2, Kd: 530 nM

 		99%+
CI-1040 ++

MEK1, IC50: 17 nM

 		++

MEK2, IC50: 17 nM

 		99%+
Myricetin ✔ 98%
Refametinib ++

MEK1, IC50: 19 nM

 		++

MEK2, IC50: 47 nM

 		99%+
Cobimetinib +++

MEK1, IC50: 4.2 nM

 		99%+
PD98059 +

MEK1, IC50: 2 μM

 		99%+
SL327 +

MEK1, IC50: 0.18 μM

 		+

MEK2, IC50: 0.22 μM

 		AP-1 98+%
PD318088 ✔ 98%
AZD8330 +++

MEK1/2, IC50: 7 nM

 		99%+
Pimasertib 98%
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

 		99%+
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Trametinib 生物活性

靶点

  • MEK2

    MEK2, IC50:1.8 nM

  • MEK1

    MEK1, IC50:0.92 nM
描述 Trametinib, also called as GSK1120212 or JTP-74057, can strongly inhibit MEK1/2 kinase activities with IC50 value of 0.92nM and 1.8nM, respectively, without inhibition on the other 98 kinases (measured by Raf-MEK-ERK cascade kinase assay) regardless of the isotype of Raf and MEK. Trametinib can inhibit constitutive ERK phosphorylation (downstream of MEK) in cell lines, while the effect on anti-proliferation differs. Among them, HT-29 and COLO205 cells with a constitutively active B-Raf mutant were most sensitive to trametinib while COLO320 DM cells bearing the wild-type gene in both B-Raf and K-Ras were found to be resistant to trametinib. Oral treatment of trametinib 1mg/kg daily for 14 days blocked the tumor increase almost completely in nude mice bearing the HT-29 xenografts[1].Trametinib is indicated for the treatment in patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations detected by an FDA-approved test[2].
作用机制 Trametinib binds to MEK1/2 and induces allosteric inhibition of MEK1/2 catalysis.[3]

Trametinib 动物研究

Dose Mice: min = 0.3 mg/kg[1], max = 2 mg/kg[2]
Administration p.o.

Trametinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03225664 Lung Diseases Due to External ... 展开 >>Agents Non-Small Cell Lung Cancer 收起 << Phase 1 Phase 2 Recruiting May 2020 United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Clinical Research Operations       CR_Study_Registration@mdanderson.org 收起 <<
NCT02872259 Melanoma Phase 1 Phase 2 Recruiting March 2020 Norway ... 展开 >> Haukeland University Hospital Recruiting Bergen, Norway, 5021 Contact: Oddbjørn Straume, MD, PhD       oddbjorn.straume@helse-bergen.no    Akershus Univerisity Hospital Not yet recruiting Lørenskog, Norway, 1478 Contact: Jürgen Geisler, MD, PhD       Jurgen.geisler@ahus.no    Oslo University Hospital, Radiumhospitalet Recruiting Oslo, Norway, 0424 Contact: Marta Nyakas, MD, PhD       marta.nyakas@ous.no    University Hospital of North Norway Recruiting Tromsø, Norway, 9038 Contact: Anita Amundsen, MD       Anita.amundsen@unn.no    St. Olavs Hospital Recruiting Trondheim, Norway, 7006 Contact: Jarle Karlsen, MD       Jarle.Karlsen@stolav.no 收起 <<
NCT02039947 Melanoma and Brain Metastases Phase 2 Completed - -

Trametinib 参考文献

[1]Fujishita T, Kajino-Sakamoto R, et al. Antitumor activity of the MEK inhibitor trametinib on intestinal polyp formation in Apc(Δ716) mice involves stromal COX-2. Cancer Sci. 2015 Jun;106(6):692-9.

[2]Kawaguchi K, Igarashi K, et al. MEK inhibitors cobimetinib and trametinib, regressed a gemcitabine-resistant pancreatic-cancer patient-derived orthotopic xenograft (PDOX). Oncotarget. 2017 Jul 18;8(29):47490-47496.

[3]Walters DM, Lindberg JM, et al. Inhibition of the growth of patient-derived pancreatic cancer xenografts with the MEK inhibitor trametinib is augmented by combined treatment with the epidermal growth factor receptor/HER2 inhibitor lapatinib. Neoplasia. 2013;15(2):143-55.

[4]Ganesh S, Shui X, et al. β-Catenin mRNA Silencing and MEK Inhibition Display Synergistic Efficacy in Preclinical Tumor Models. Mol Cancer Ther. 2018;17(2):544-553.

Trametinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.62mL

0.33mL

0.16mL

8.12mL

1.62mL

0.81mL

16.25mL

3.25mL

1.62mL

Trametinib 技术信息

CAS号871700-17-3
分子式C26H23FIN5O4
分子量 615.395
别名 JTP-74057;GSK1120212;Trametinib. Brand name: Mekinist.;GSK 1120212 GSK1120212
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 25 mg/mL(40.62 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

Tags: Trametinib | 871700-17-3 | GSK1120212 | JTP-74057 | GSK 1120212 | GSK-1120212 | JTP74057 | JTP 74057 | JTP-74057 | MEK Inhibitor | MAPK/ERK Pathway | Autophagy | Apoptosis | MEK | Autophagy | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Trametinib 纯度/质量文件 | Trametinib 亚型比较 | Trametinib 生物活性 | Trametinib 动物研究 | Trametinib 临床数据 | Trametinib 参考文献 | Trametinib 实验方案 | Trametinib 技术信息

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