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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $43 | In Stock | |
2 mg | $60 | In Stock | |
5 mg | $113 | In Stock | |
10 mg | $206 | In Stock | |
25 mg | $442 | In Stock | |
50 mg | $575 | In Stock | |
100 mg | $683 | In Stock | |
500 mg | $1,450 | In Stock |
Description | 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. |
Targets&IC50 | c-Met:4 nM |
In vitro | 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] |
In vivo | 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] |
Alias | MSC2156119, EMD-1214063 |
Molecular Weight | 492.57 |
Formula | C29H28N6O2 |
Cas No. | 1100598-32-0 |
Smiles | CN1CCC(COc2cnc(nc2)-c2cccc(Cn3nc(ccc3=O)-c3cccc(c3)C#N)c2)CC1 |
Relative Density. | 1.25 g/cm3 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 5.25 mg/mL (10.66 mM), Sonication is recommended. ![]() Ethanol: < 1 mg/mL (insoluble or slightly soluble) | ||||||||||||||||||||
In Vivo Formulation | 5% DMSO+95% (20% SBE-β-CD in Saline): 2 mg/mL (4.06 mM), Suspension. In vivo: 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. ![]() 0.5% CMC-Na: 2 mg/mL (4.06 mM), Suspension ![]() 10% DMSO+90% Saline: 0.27 mg/mL (0.55 mM), In vivo: 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. Please add the 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. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.![]() | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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