Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 43.00 | |
2 mg | In stock | $ 60.00 | |
5 mg | In stock | $ 113.00 | |
10 mg | In stock | $ 206.00 | |
25 mg | In stock | $ 442.00 | |
50 mg | In stock | $ 575.00 | |
100 mg | In stock | $ 683.00 | |
500 mg | In stock | $ 1,450.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 122.00 |
Description | Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. |
Targets&IC50 | c-Met:4 nM |
In vitro | EMD 1214063 inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with EMD 1214063 induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. EMD 1214063 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. EMD 1214063 considerably inhibits the viability of MKN-45 cells with IC50 of less than 1 nM. Treatment with EMD 1214063 (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 | EMD 1214063 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. EMD 1214063 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 EMD 1214063. EMD 1214063 (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] |
Synonyms | EMD-1214063, MSC2156119 |
Molecular Weight | 492.57 |
Formula | C29H28N6O2 |
CAS No. | 1100598-32-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 1mg/ml
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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Tepotinib 1100598-32-0 Tyrosine Kinase/Adaptors Trk receptor c-Met/HGFR TAM Receptor EMD-1214063 EMD 1214063 MSC2156119 EMD1214063 MSC-2156119 MSC 2156119 inhibitor inhibit