1100598-32-0
Chemical Structure
Tepotinib
Synonym(s): EMD-1214063
- CAS No.: 1100598-32-0
- Formula:C29H28N6O2
- Molecular Weight:492.57
IUPAC Name: 3-(1-(3-(5-((1-methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile
InChIKey: AHYMHWXQRWRBKT-UHFFFAOYSA-N
SMILES: N#CC1=CC=CC(C(C=CC2=O)=NN2CC3=CC=CC(C4=NC=C(C=N4)OCC5CCN(CC5)C)=C3)=C1
Biological Activity: Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Tepotinib | 99.94% | Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects. | ||||||||||||||||||||
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Tepotinib (Standard) | 98.44% | Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects. | ||||||||||||||||||||
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Tepotinib-d5 | Octacosanoic acid-d35 is the deuterated-labeled Octacosanoic acid. Octacosanoic acid (Montanic acid) is a long-chain saturated fatty acid and a major component of sugarcane wax mixture and D-003. Octacosanoic acid can be formed in the liver from Octacosanol (HY-N6811) and inhibits nitric oxide (NO) production in LPS-activated macrophages and LPS-induced splenic lymphocyte proliferation. Octacosanoic acid can be used in anti-inflammatory and lipid metabolism-related research. | |||||||||||||||||||||
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Tepotinib-13C,d3 | Tepotinib-13C,d3 (EMD-1214063-13C,d3) is the 13C, deuterated-labeled Tepotinib (HY-14721). Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects. | |||||||||||||||||||||
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Tepotinib-d3 | Tepotinib-d3 (EMD-1214063-d3) is the deuterated-labeled Tepotinib (HY-14721). Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects. | |||||||||||||||||||||
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References
- [1]. Bladt F, et al. EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res, 2013, 19(11), 2941-2951. [Content Brief]
- [2]. Zhan N, et al. The Effect of Selective c-MET Inhibitor on Hepatocellular Carcinoma in the MET-Active, β-Catenin-Mutated Mouse Model. Gene Expr. 2018 May 18;18(2):135-147. [Content Brief]
- [3]. A. Naing, et al. IS4-1 - A Phase I Dose-Escalation Study of emd 1214063, an Oral Selective CMET Inhibitor, in Patients with Advanced Solid Tumors. Annals of Oncology. Volume 23, Supplement 11, October 2012, Page xi21.
