Tepotinib NEW
| Price | $43 | $60 | $113 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-13 |
Product Details
| Product Name: Tepotinib | CAS No.: 1100598-32-0 |
| Purity: 99.81% | Supply Ability: 10g |
| Release date: 2024/11/13 |
Product Introduction
Bioactivity
| 名稱(chēng) | Tepotinib |
| 描述 | Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer. |
| 體外活性 | Tepotinib inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with Tepotinib induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. Tepotinib effectively blocka phosphorylation of the major downstream effectors of the c-Met enzyme, such as Grb2, Gab1, Sos, PLCγ, and phosphoinositide 3-kinase, in EBC-1, MKN-45, and Hs746T cells in the range of 1 to 10 nM. Tepotinib considerably inhibits the viability of MKN-45 cells with IC50 of less than 1 nM. Treatment with Tepotinib (as low as 0.1 nM) inhibits HGF-induced NCI-H441 cell migration, whereas concentrations of 100 nM to 1 μM almost completely prevents it. [1] |
| 體內(nèi)活性 | Tepotinib treatment, at doses of 10 mg/kg or more, results in more than 90% inhibition of c-Met phosphorylation in Hs746T xenograft tumor for a period of at least 72 hours. Tepotinib induces more than 50% reduction of cyclin D1 expression, which persists after 96 hours upon treatment with doses of 100 mg/kg. A transient induction of p27 and cleaved caspase-3 are also observed upon treatment with Tepotinib. Tepotinib (15 mg/kg, daily) treatment induces complete regression of gastric carcinoma xenografts Hs746T, in which c-Met is amplified, overexpressed, and activated in a ligand-independent fashion. [1] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 1 mg/mL Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+90% Saline : 0.27 mg/mL (0.55 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. |
| 關(guān)鍵字 | Tepotinib | EMD 1214063 | EMD1214063 | MSC-2156119 | MSC 2156119 |
| 相關(guān)產(chǎn)品 | Gilteritinib | Larotrectinib sulfate | L-Ascorbic acid 2-phosphate trisodium | Crizotinib | Amitriptyline hydrochloride | 7,8-Dihydroxyflavone | Diosmetin | GW 441756 | Cabozantinib S-malate |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | 激酶抑制劑庫(kù) | 抗癌上市藥物庫(kù) | FDA 上市激酶抑制劑庫(kù) | FDA 上市藥物庫(kù) | 已知活性化合物庫(kù) | 抗癌藥物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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