Catalog No. A3018
Trametinib (GSK1120212)(别名:Trametinib, 曲美替尼)
MEK1和MEK2抑制剂
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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥500.00 | 现货 | |
50mg | ¥872.00 | 现货 | |
200mg | ¥1745.00 | 现货 | |
500mg | ¥3681.00 | 现货 |
CAS号:871700-17-3纯度:98.14%
仅用于科研,不用于诊疗。未经明确授权不得转售。
A
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特色产品
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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
- 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)](/_next/image?url=https%3A%2F%2Fresource.apexbio.cn%2Fapexbio%2Fbanner%2FK1079-K1081_1.png&w=3840&q=75)
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
- 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
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 |
SMILES | CC1=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 |
SDF文件 | Download SDF |
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 | MEK1 | MEK2 |
生物活性数据 | 0.92 nM | 1.8 nM |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. 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
- 2. 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
- 3. 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
- 4. 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
- 5. 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
- 6. 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
- 7. 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
- 8. 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
- 9. 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
- 10. 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
- 11. 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
- 12. 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
- 13. 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
- 14. Juliane Buhl. "The senescence-associated secretory phenotype regulates the growth behavior of pediatric pilocytic astrocytoma." Ruperto Carola University Heidelberg. 2018.
- 15. 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
- 16. 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
- 17. 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
- 18. 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
- 19. 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
- 20. 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
- 21. 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
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