Tepotinib hydrochloride
Based on 8 publication(s) in Google Scholar
Tepotinib (EMD-1214063) hydrochloride 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 hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects.
For research use only. We do not sell to patients.
- CAS No.: 1103508-80-0
- Formula: C29H28N6O2.xHCl
- Molecular Weight:492.57 (free base)
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tepotinib hydrochloride
More- Nat Biotechnol. 2026 Apr 20. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Adv. 2020 Aug 21;6(34):eaba8968. [Abstract]
- Int J Biol Macromol. 2025 Apr 12:143133. [Abstract]
- Int J Biol Macromol. 2023 Jun 30:241:124656. [Abstract]
- Separations. 2023 May 26, 10(6), 330.
- medRxiv. 2026 May 6:2026.05.05.26352474. [Abstract]
- Gene Expr. 2018 May 18;18(2):135-147. [Abstract]
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Biological Activity
Tepotinib hydrochloride inhibits IRAK4, TrkA, Axl, IRAK1, Mer, and TrkA with IC50s of 615, 1017, 1566, 2037, 2272, and 5716 nM, respectively[1].
Tepotinib hydrochloride inhibits HGF-induced c-Met phosphorylation, with an average IC50 of 6 nM in A549 cells[1].
Tepotinib (0.01 nM-30 μM) hydrochloride inhibits tumor cell proliferation and migration in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 or BALB/C nude mice bearing human cancer cell lines KP-4, or EBC-1[1]
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Dosage:6 and 15 mg/kg for mice bearing NSCLC EBC-1; 25, 50 and 200 mg/kg for mice bearing pancreatic carcinoma cell line KP-4.
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Administration:Injected daily; for 14-18 days
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Result:Daily administration of 5 or 15 mg/kg to EBC-1 tumor-bearing mice resulted in effective inhibition or complete tumor regression, respectively.
Induced dose-dependent tumor growth inhibition in mice bearing human pancreatic carcinoma KP-4 tumors.
Chemical Information
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CAS No. 1103508-80-0
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Molecular Weight 492.57 (free base)
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Formula C29H28N6O2.xHCl
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SMILES
N#CC1=CC=CC(C(C=CC2=O)=NN2CC3=CC=CC(C4=NC=C(C=N4)OCC5CCN(CC5)C)=C3)=C1.[H]Cl.[x]
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Synonyms
EMD-1214063 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Biotechnol
Comprehensive profiling of clinically approved kinase inhibitors reveals mutation-specific inhibitors and opportunities for drug repurposing. [Abstract]2026 Apr 20. PMID: 42010121 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Adv
Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis. [Abstract]2020 Aug 21;6(34):eaba8968. PMID: 32937365 -
Int J Biol Macromol
Tepotinib interaction triggers a slight effect on the overall stability of hemoglobin protein, reinforcing the potential suitability as a drug candidate against gastric cancer. [Abstract]2025 Apr 12:143133. PMID: 40228765 -
Int J Biol Macromol
Elucidation of binding dynamics of tyrosine kinase inhibitor tepotinib, to human serum albumin, using spectroscopic and computational approach. [Abstract]2023 Jun 30:241:124656. PMID: 37119913 -
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medRxiv
A liver-heart endocrine axis revealed by systems genetics and mediated by hepatocyte growth factor activator. [Abstract]2026 May 6:2026.05.05.26352474. PMID: 42145616 -
Gene Expr
The Effect of Selective c-MET Inhibitor on Hepatocellular Carcinoma in the MET-Active, β-Catenin-Mutated Mouse Model. [Abstract]2018 May 18;18(2):135-147. PMID: 29409568
Tepotinib hydrochloride purchased from MedChemExpress. Usage Cited in: Gene Expr. 2018 May 18;18(2):135-147. [Abstract]
Western blot for Myc-tag shows decrease in Myc-tag levels at 8 weeks of EMD1214063 treatment only. GAPDH shows comparable loading in all lanes.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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