product name Tepotinib (EMD 1214063)
Description: Tepotinib (also known as EMD 1214063) is a potent and selective c-Met inhibitor with IC50 of 4 nM, and is >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib can inhibit HGF-induced c-Met phosphorylation with an average IC50 of 6 nM in A549 cells. It also significantly inhibits the activation of downstream signaling pathways of c-Met including the phosphorylation of Akt, Gab-1and Erk1/2.
References: Clin Cancer Res. 2013 Jun 1;19(11):2941-51.
492.57
Formula
C29H28N6O2
CAS No.
1100598-32-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (10.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+corn oil: 5mg/mL
Synonyms
EMD 1214063, MSC2156119
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19402588
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Cancer Res. 2013 Jun 1;19(11):2941-51 |
Related Posts
product name Tepotinib (EMD 1214063)
Description: Tepotinib (also known as EMD 1214063) is a potent and selective c-Met inhibitor with IC50 of 4 nM, and is >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib can inhibit HGF-induced c-Met phosphorylation with an average IC50 of 6 nM in A549 cells. It also significantly inhibits the activation of downstream signaling pathways of c-Met including the phosphorylation of Akt, Gab-1and Erk1/2.
References: Clin Cancer Res. 2013 Jun 1;19(11):2941-51.
492.57
Formula
C29H28N6O2
CAS No.
1100598-32-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL (10.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
5% DMSO+corn oil: 5mg/mL
Synonyms
EMD 1214063, MSC2156119
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19402588
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Cancer Res. 2013 Jun 1;19(11):2941-51 |