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Tepotinib

Catalog No. T6121 CAS 1100598-32-0

Synonyms: EMD-1214063, MSC2156119

Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity.

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Tepotinib, CAS 1100598-32-0

Pack Size	Availability	Price/USD
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

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Purity: 99.81%

Purity: 98.84%

Purity: 98.37%

Purity: 98.35%

Purity: 98.2%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Bladt F, et al. Clin Cancer Res, 2013, 19(11), 2941-2951.

Citations

1. Li P, Jia C, Fan Z, et al.Discovery of novel exceptionally potent and orally active c-MET PROTACs for the treatment of tumors with MET alterations.Acta Pharmaceutica Sinica B.2023

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library EMA Approved Drug Library Anti-Cancer Drug Library FDA-Approved Kinase Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library

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Related compounds with same targets

LM22A-4 Trk-IN-4 LM22B-10 Protein kinase inhibitor 5 sulfate hydrate BMS-754807 Repotrectinib LOXO-195 Sitravatinib

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Keywords

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

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