Size | Price | |
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Discontinued |
Purity: ≥98%
This product has been discontinued. Tepotinib (formerly EMD 1214063, EMD-1214063; MSC2156119; MSC-2156119; Tepmetko) is a selective c-Met inhibitor with potential antineoplastic activity. Tepotinib has been approved for the treatment of adults with metastatic non-small cell lung cancer whose tumors have a mutation that causes exon 14 skipping in the mesenchymal-epithelial transition in 2020 in Japan and in the USA in 2021. With an IC50 of 4 nM, it exhibits >200-fold selectivity in inhibiting c-Met relative to other kinases, including IRAK4, TrkA, Axl, IRAK1, and Mer. In A549 cells, tecitinib has an average IC50 of 6 nM to suppress HGF-induced c-Met phosphorylation. Moreover, it strongly suppresses the phosphorylation of Akt, Gab-1, and Erk1/2, as well as the activation of downstream signaling pathways of c-Met.
Targets |
c-Met (IC50 = 4 nM)
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ln Vitro |
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ln Vivo |
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Cell Assay |
Tepotinib (EMD-1214063) is a c-Met inhibitor that is both potent and selective. With an IC50 of 4 nM, it is >200 times more selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer.
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Animal Protocol |
Human gastric carcinoma xenografts Hs746T
15 mg/kg daily |
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References |
Molecular Formula |
C29H28N6O2
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Molecular Weight |
492.57
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Exact Mass |
492.22737416
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CAS # |
1100598-32-0
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SMILES |
CN1CCC(CC1)COC2=CN=C(N=C2)C3=CC=CC(=C3)CN4C(=O)C=CC(=N4)C5=CC=CC(=C5)C#N
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InChi Key |
AHYMHWXQRWRBKT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C29H28N6O2/c1-34-12-10-21(11-13-34)20-37-26-17-31-29(32-18-26)25-7-3-5-23(15-25)19-35-28(36)9-8-27(33-35)24-6-2-4-22(14-24)16-30/h2-9,14-15,17-18,21H,10-13,19-20H2,1H3
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Chemical Name |
3-[1-[[3-[5-[(1-methylpiperidin-4-yl)methoxy]pyrimidin-2-yl]phenyl]methyl]-6-oxopyridazin-3-yl]benzonitrile
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Synonyms |
EMD-1214063; MSC-2156119; EMD1214063; EMD 1214063; MSC2156119; MSC 2156119; Tepotinib
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0302 mL | 10.1508 mL | 20.3017 mL | |
5 mM | 0.4060 mL | 2.0302 mL | 4.0603 mL | |
10 mM | 0.2030 mL | 1.0151 mL | 2.0302 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03940703 | Active Recruiting |
Drug: Tepotinib Drug: Osimertinib |
Non-small Cell Lung Cancer | EMD Serono Research & Development Institute, Inc. |
September 19, 2019 | Phase 2 |
NCT02864992 | Active Recruiting |
Drug: Tepotinib | Lung Adenocarcinoma Stage IIIB/IV Amplification |
EMD Serono Research & Development Institute, Inc. |
September 13, 2016 | Phase 2 |
NCT05120960 | Recruiting | Drug: tepotinib plus osimertinib Drug: tepotinib |
Brain Tumor | M.D. Anderson Cancer Center | February 27, 2023 | Phase 1 |
NCT04647838 | Recruiting | Drug: Tepotinib | Solid Tumor MET Amplification |
Chungbuk National University Hospital |
January 16, 2020 | Phase 2 |
NCT05782361 | Recruiting | Drug: Tepotinib Drug: Pembrolizumab |
Non Small Cell Lung Cancer Advanced Cancer |
Institute of Cancer Research, United Kingdom |
May 3, 2023 | Phase 1 |
Dose-dependent inhibition of c-Met auto-phosphorylation in vivo. Clin Cancer Res. 2013 Jun 1;19(11):2941-51. td> |
EMD 1214063 and EMD 1204831 effectively inhibit tumor c-Met auto-phosphorylation and cyclin D1 expression while inducing p27 expression. Clin Cancer Res. 2013 Jun 1;19(11):2941-51. td> |
EMD 1214063 and EMD 1204831 display antitumor activity in HGF-dependent and HGF-independent xenograft tumor models. Clin Cancer Res. 2013 Jun 1;19(11):2941-51. td> |