登录/注册

Catalog No. A3018

Trametinib (GSK1120212)

（别名：Trametinib, 曲美替尼）
MEK1和MEK2抑制剂
Trametinib (GSK1120212)
规格价格货期数量
1mL(10 mM in DMSO)
￥425.00
现货
50mg
￥726.00
现货
200mg
￥1375.00
现货
500mg
￥3094.00
现货
CAS号：871700-17-3纯度：99.33%
仅用于科研，不用于诊疗。未经明确授权不得转售。
A
021-55669583sales@apexbio.cnAPExBIO

特色产品

Annexin V-FITC/PI Apoptosis Kit
Annexin V-FITC/PI Apoptosis Kit
用于双染检测细胞凋亡和坏死
- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
Phos binding reagent (Phosbind) acrylamide
Phos binding reagent (Phosbind) acrylamide
分离和检测磷酸化/非磷酸化蛋白
- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
Cell Counting Kit-8 (CCK-8)
Cell Counting Kit-8 (CCK-8)
用于细胞增殖和细胞毒性试验
- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
Cy5 TSA Fluorescence System Kit
Cy5 TSA Fluorescence System Kit
Cy5荧光标记的酪胺信号放大系统
- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)
EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)
用于观察mRNA运送，定位，翻译
- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
HotStart™ 2X Green qPCR Master Mix
HotStart™ 2X Green qPCR Master Mix
用于荧光定量目标DNA或cDNA
- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus
HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus
高效的Cy5修饰RNA转录试剂盒
- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述

Trametinib（GSK1120212，JTP 74057）最初被鉴定是一个p15感应性的化合物，是一种新型有效的MEK激酶抑制剂，以ATP非竞争性的方式抑制MEK1和MEK2。据报道，Trametinib在多种肿瘤异种移植模型（包括HT-29和COLO205结直肠肿瘤细胞系）中展示了广泛的抗肿瘤活性。在HT-29细胞中，Trametinib诱导p15和p27的表达，减少细胞周期蛋白D1的水平，引起RB蛋白的去磷酸化和G1期停滞，并减少TS的表达。在含有B-RAF突变的肿瘤细胞系中，Trametinib也可以有效的抑制ERK 1/2的磷酸化，从而导致细胞生长抑制。

参考文献：
Akintunde Akinleye, Muhammad Furqan, Nikhil Mukhi, Pavan Ravella and Delong Liu.  MEK and the inhibitors: from bench to bedside. Journal of Hematology & Oncology 2013, 6:27
Motoki Watanabe, Yoshihiro Sowa, Mayumi Yogosawa and Toshiyuki Sakai.  Novel MEK inhibitor trametinib and other retinoblastoma gene (RB)-reactivating agents enhance efficacy of 5-fluorouracil on human colon cancer cells. Cancer Sci 2013; 104(6): 687-693

产品性质

物理外观A solid
CAS号871700-17-3
分子式C26H23FIN5O4
分子量615.39
小分子别名Trametinib
化学名称N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide
溶解度insoluble in H2O; insoluble in EtOH; ≥15.38 mg/mL in DMSO
SMILESCC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5
存储条件-20°C
运输条件蓝冰

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述Trametinib (GSK1120212)是一个高度特异性的、有效的MEK1/2抑制剂，IC50值为0.92 nM/1.8 nM。
靶点MEK1MEK2
生物活性数据0.92 nM1.8 nM

生物相关数据

质量控制

请选择批次查看:
纯度 = 99.33%
COAHPLCNMRMSDS

操作说明

小分子化合物通用使用指南Datasheet

APExBIO 顾客使用本产品发表的 30 篇科研文献

1. Charlie George Barker, Sumana Sharma, et al. "Integrative multi-omics defines melanoma drug response networks and ARID1A-dependent resistance mechanisms." Mol Syst Biol. 2026 Feb 18. PMID: 41708984

2. Milad Mohammadi, Maike Siobal, Jörg Isensee. "BH4 Oxidation‐Derived H2O2 Activates ERK1/2 Signaling via B‐Raf in Rat Dorsal Root Ganglion Neurons." J Neurochem. 2025 Nov 3;169(11):e70271. PMID: 41178527

3. Michelle C Barbeau, Brooke A Brown, Sara J Adair. "The kinase ERK plays a conserved dominant role in the heterogeneity of epithelial-mesenchymal transition in pancreatic cancer cells." Sci Signal . 2025 Aug 12;18(899):eads7002. PMID: 40794842

4. Karolina Borankova, Matyas Solny, et al. "Depletion of chemoresponsive mitochondrial fission mediator DRP1 does not mitigate sarcoma resistance." Life Sci Alliance. 2024 Dec 6;8(2):e202402870. PMID: 39643272

5. Haoyang Zhuang, Shuhong Han, et al. "MEK1/2 and ERK1/2 mediated lung endothelial injury and altered hemostasis promote diffuse alveolar hemorrhage in murine lupus." bioRxiv. 2024 May 10:2024.05.07.593006. PMID: 38766226

6. Yunseong Kim, Younghyun Han, et al. "A gray box framework that optimizes a white box logical model using a black box optimizer for simulating cellular responses to perturbations." Cell Rep Methods. 2024 May 20;4(5):100773. PMID: 38744288

7. Wei Li, Masha Huang, et al. "mRNA-Lipid Nanoparticle-Mediated Restoration of PTPN14 Exhibits Antitumor Effects by Overcoming Anoikis Resistance in Triple-Negative Breast Cancer." Advanced Science. Volume11, Issue 32 August 27, 2024 2309988

8. Spandana Kotian, Lindsay F. Rizzardi, et al. "MEK1/2 kinases cooperate with c-Myc:MAX to prevent polycomb repression of TERT in human pluripotent stem cells." September 18, 2024

9. Josh L. Stern, Lindsay F. Rizzardi, et al. "Apurinic/apyrimidinic endodeoxyribonuclease 2 (APEX2/APE2) is required for efficient expression of TERT in human embryonic stem cells." September 23, 2024

10. Junli Wang, Sijia Weng, et al. "PKCι induces differential phosphorylation of STAT3 to modify STAT3-related signaling pathways in pancreatic cancer cells." J Cell Commun Signal. 2023 Aug 7. PMID: 37548811

11. Paul J Myers, Sung Hyun Lee, et al. "An integrated mechanistic and data-driven computational model predicts cell responses to high-and low-affinity EGFR ligands." bioRxiv. 2023 Jun 26:2023.06.25.543329. PMID: 37425852

12. Xiaofei Zhang, Tiebo Mao, et al. "Synergistic blocking of RAS downstream signaling and epigenetic pathway in KRAS mutant pancreatic cancer." Aging (Albany NY). 2022 Apr 25;14(8):3597-3606. PMID: 35468095

13. Wendy S. Chen, Yan Liang, et al. "Single-cell transcriptomics reveals opposing roles of Shp2 in Myc-driven liver tumor cells and microenvironment." Cell Rep. 2021 Nov 9;37(6):109974. PMID: 34758313

14. Heng-Huan Lee, Ying-Nai Wang, et al. "Human ribonuclease 1 serves as a secretory ligand of ephrin A4 receptor and induces breast tumor initiation." Nat Commun. 2021 May 13;12(1):2788. PMID: 33986289

15. Gabriele Manzella, Leonie D. Schreck, et al. "Phenotypic profiling with a living biobank of primary rhabdomyosarcoma unravels disease heterogeneity and AKT sensitivity." Nature Communications volume 11, Article number: 4629 (2020) PMID: 32934208

16. Xu WF, Wang ZJ, et al. "Huai Qi Huang-induced Apoptosis via Down-regulating PRKCH and Inhibiting RAF/MEK/ERK Pathway in Ph+ Leukemia Cells." Curr Med Sci. 2020;40(2):354-362. PMID: 32337697

17. Day EK, Sosale NG, et al. "Glioblastoma Cell Resistance to EGFR and MET Inhibition Can Be Overcome via Blockade of FGFR-SPRY2 Bypass Signaling." Cell Rep. 2020;30(10):3383-3396.e7. PMID: 32160544

18. Park SM, Hwang CY, et al. "Feedback analysis identifies a combination target for overcoming adaptive resistance to targeted cancer therapy." Oncogene. 2020;39(19):3803-3820. PMID: 32157217

19. Challa S, Husain K, et al. "Targeting the IκB Kinase Enhancer and Its Feedback Circuit in Pancreatic Cancer." Transl Oncol. 2020;13(2):481–489. PMID: 32004866

20. Ruibin Bai, Yajie Zhang, et al. "Isolation, characterization and immunomodulatory activity of oligosaccharides from Codonopsis pilosula." Journal of Functional Foods. Volume 72, September 2020, 104070

21. Satoh TK, Mellett M, et al. "IL-36γ drives skin toxicity induced by EGFR/MEK inhibition and commensal Cutibacterium acnes." J Clin Invest. 2019 Dec 5. pii: 128678. PMID: 31805013

22. Roche SL, Kutsyr O, et al. "Norgestrel, a Progesterone Analogue, Promotes Significant Long-Term Neuroprotection of Cone Photoreceptors in a Mouse Model of Retinal Disease." Invest Ophthalmol Vis Sci. 2019 Jul 1;60(8):3221-3235. PMID: 31335948

23. Cho SY, Chae J, et al. "Unstable Genome and Transcriptome Dynamics during Tumor Metastasis Contribute to Therapeutic Heterogeneity in Colorectal Cancers." Clin Cancer Res. 2019 Jan 22. PMID: 30670495

24. Buhl JL, Selt F, et al. "The senescence-associated secretory phenotype mediates oncogene-induced senescence in pediatric pilocytic astrocytoma." Clin Cancer Res. 2018 Dec 7. pii: clincanres.1965.2018. PMID: 30530705

25. Knickelbein K, Tong J, et al. "Restoring PUMA induction overcomes KRAS-mediated resistance to anti-EGFR antibodies in colorectal cancer." Oncogene. 2018 May 14. PMID: 29755130

26. Wang YN, Lee HH, et al. "Angiogenin/Ribonuclease 5 Is an EGFR Ligand and a Serum Biomarker for Erlotinib Sensitivity in Pancreatic Cancer." Cancer Cell. 2018 Apr 9;33(4):752-769.e8. PMID: 29606349

27. Hogstad B, Berres ML, et al. "RAF/MEK/extracellular signal-related kinase pathway suppresses dendritic cell migration and traps dendritic cells in Langerhans cell histiocytosis lesions." J Exp Med. 2018 Jan 2;215(1):319-336. PMID: 29263218

28. Juliane Buhl. "The senescence-associated secretory phenotype regulates the growth behavior of pediatric pilocytic astrocytoma." Ruperto Carola University Heidelberg. 2018

29. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID: 29249695

30. Yong LK, Lai S, et al. "Overexpression of Semaphorin-3E enhances pancreatic cancer cell growth and associates with poor patient survival." Oncotarget. 2016 Dec 27;7(52):87431-87448. PMID: 27911862

摩尔浓度计算器

质量
= 浓度
x 体积
x 分子量
*在配置溶液时，请务必参考产品标签上、MSDS / COA（可在Apexbio的产品页面获得）批次特异的分子量使用本工具。

相关产品

Z-VAD-FMK
A1902 Z-VAD-FMK
MG-132
A2585 MG-132
Q-VD-OPh
A1901 Q-VD-OPh
Ferrostatin-1 (Fer-1)
A4371 Ferrostatin-1 (Fer-1)
Rapamycin (Sirolimus)
A8167 Rapamycin (Sirolimus)
LY 294002
A8250 LY 294002
Bromodomain Inhibitor, (+)-JQ1
A1910 Bromodomain Inhibitor, (+)-JQ1
Bortezomib (PS-341)
A2614 Bortezomib (PS-341)
ABT-263 (Navitoclax)
A3007 ABT-263 (Navitoclax)
MK-2206 dihydrochloride
A3010 MK-2206 dihydrochloride
产品目录
产品目录
质量认证
产品目录
订单信息
客户支持
联系我们
通讯
获取最新资讯，产品折扣和优惠。
Copyright ©2013-2026 APExBIO Technology. All Rights Reserved.沪公网安备 31011002003500沪公网安备 31011002003500沪ICP备14019579号-3