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Submit ReviewTrametinib
说明： Potent and selective MEK inhibitor; orally bioavailable
化学名： N-[3-[3-Cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-3,4,6,7-tetrahydro-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl]acetamide
纯度： ≥98% (HPLC)
生物活性 for Trametinib
Trametinib is a potent and selective MEK1 and MEK2 inhibitor (IC50 = 0.92 and 1.8 nM, respectively, in cell-free assays). In vitro, it inhibits the growth of human colorectal cancer cell lines expressing either B-RAF or K-RAF (IC50 values range from 0.48 to 36 nM). In vivo, it suppresses tumor growth of HT-29 and COLO205 xenografts in nude mice. Trametinib induces apoptosis. This compound is orally bioavailable.
化合物库 for Trametinib
Trametinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Trametinib
| 分子量 | 615.4 |
| 公式 | C26H23FIN5O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 871700-17-3 |
| PubChem ID | 11707110 |
| InChI Key | LIRYPHYGHXZJBZ-UHFFFAOYSA-N |
| Smiles | O=C(NC1=CC=CC(=C1)N2C(=O)N(C(=O)C3=C(NC4=CC=C(I)C=C4F)N(C(=O)C(=C32)C)C)C5CC5)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Trametinib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 61.54 | 100 |
制备储备液 for Trametinib
以下数据基于产品分子量 615.4。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.62 mL | 8.12 mL | 16.25 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.25 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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产品说明书 for Trametinib
参考文献 for Trametinib
参考文献是支持产品生物活性的出版物。
Yamaguchi et al (2011) Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int.J.Oncol. 39 23 PMID: 21523318
Kobelt et al (2021) The newly identified MEK1 tyrosine phosphorylation target MACC1 is druggable by approved MEK1 inhibitors to restrict colorectal cancer metastasis. Oncogene 40 5286 PMID: 34247190
Zhao et al (2021) Diverse alterations associated with resistance to KRAS(G12C) inhibition. Nature 599 679 PMID: 34759319
If you know of a relevant reference for Trametinib, please let us know.
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关键词: Trametinib, Trametinib supplier, Potent, inhibitors, inhibits, MEK1, MEK2, MEK, Mitogen-Activated, Protein, Kinase, Kinases, orally, bioavailable, 7709, Tocris Bioscience
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Trametinib 的评论
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for Trametinib
