Cat. No.: HY-14721

Tepotinib

(Synonyms: EMD-1214063)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

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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Pureté: 99.94%
CAS No.: 1100598-32-0
Formule: C₂₉H₂₈N₆O₂
Masse moléculaire:492.57

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tepotinib Chemical Structure

CAS No.: 1100598-32-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

c-Met

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	12 nM Compound: 22	Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay	[PMID: 25736998]
AGS	IC₅₀	1448 nM Compound: 3; T6121	Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	1.5 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein H1094Y mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein H1094Y mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	10 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200L mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200L mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	1835 nM Compound: Tepotinib	Antiproliferative activity against mouse BaF3 cells harboring TPR-MET Y1230H mutant fusion protein incubated for 72 hrs by CellTiter-Glo reagent based assay Antiproliferative activity against mouse BaF3 cells harboring TPR-MET Y1230H mutant fusion protein incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 38962837]
BaF3	IC₅₀	2.5 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein M1250T mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein M1250T mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	2029.1 nM Compound: Tepotinib	Antiproliferative activity against mouse BaF3 cells harboring TPR-MET D1228N mutant fusion protein incubated for 72 hrs by CellTiter-Glo reagent based assay Antiproliferative activity against mouse BaF3 cells harboring TPR-MET D1228N mutant fusion protein incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 38962837]
BaF3	IC₅₀	2385 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein Y1230H mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein Y1230H mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	3055 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein D1228N mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein D1228N mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	36.6 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200I mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200I mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	46.7 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein L1195V mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein L1195V mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	5.3 nM Compound: Tepotinib	Antiproliferative activity against mouse BaF3 cells harboring TPR-MET fusion protein incubated for 72 hrs by CellTiter-Glo reagent based assay Antiproliferative activity against mouse BaF3 cells harboring TPR-MET fusion protein incubated for 72 hrs by CellTiter-Glo reagent based assay	[PMID: 38962837]
BaF3	IC₅₀	8.8 nM Compound: 3; T6121	Antiproliferative activity against mouse BaF3 cells harboring wild type Tpr-Met fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring wild type Tpr-Met fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
HepG2	IC₅₀	3.6 μM Compound: Tepotinib	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
Hs746T	IC₅₀	4.5 nM Compound: 3; T6121	Antiproliferative activity against human Hs746T cells harboring MET alterations assessed as inhibition of cell proliferation incubated for 5 days by CCK8 assay Antiproliferative activity against human Hs746T cells harboring MET alterations assessed as inhibition of cell proliferation incubated for 5 days by CCK8 assay	[PMID: 36355693]
L02	IC₅₀	10.64 μM Compound: Tepotinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
MHCC97H	IC₅₀	0.016 μM Compound: Tepotinib	Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 38716896]
MHCC97H	IC₅₀	1.18 nM Compound: Tepotinib	Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
MHCC97H	IC₅₀	3.66 nM Compound: Tepotinib	Antiproliferative activity against human MHCC97H cells incubated for 24 hrs by CCK8 assay Antiproliferative activity against human MHCC97H cells incubated for 24 hrs by CCK8 assay	[PMID: 38962837]
SNU-16	IC₅₀	363 nM Compound: 3; T6121	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay	[PMID: 36355693]

In Vitro

Tepotinib inhibits IRAK4, TrkA, Axl, IRAK1, Mer, and TrkA with IC₅₀s of 615, 1017, 1566, 2037, 2272, and 5716 nM, respectively^[1].
Tepotinib inhibits HGF-induced c-Met phosphorylation, with an average IC₅₀ of 6 nM in A549 cells^[1].
Tepotinib (0.01 nM-30 μM) 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.

Cell Viability Assay^[1]

Cell Line:

MKN-45 gastric cancer cells
Concentration:

0.01 nM, 0.03 nM, 0.1 nM, 0.3 nM, 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM and 30 μM
Incubation Time:

72 hours
Result:

Considerably inhibited the viability of MKN-45 cells with IC₅₀ values of less than 1 nM.

In Vivo

Tepotinib induces tumor regression in xenograft models and inhibits in vivo c-Met phosphorylation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CD-1 or BALB/C nude mice bearing human cancer cell lines KP-4, or EBC-1^[1]
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.
Administration:

Injected daily; for 14-18 days
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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1100598-32-0
Appearance Solid
Masse moléculaire 492.57
Formule C₂₉H₂₈N₆O₂
Color White to light yellow
SMILES

N#CC1=CC=CC(C(C=CC2=O)=NN2CC3=CC=CC(C4=NC=C(C=N4)OCC5CCN(CC5)C)=C3)=C1
Synonyms

EMD-1214063
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (9)

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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
Separations

2023 May 26, 10(6), 330.
Mol Biol Rep

Knockdown of FAXDC2 promotes cell proliferation, migration, invasion and EMT in HepG2 cells by upregulating c-Met and its phosphorylation. [Abstract]

2026 Apr 29;53(1):692. PMID: 42053668
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 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.

Solvant et solubilité

In Vitro:

DMSO : 8.75 mg/mL (17.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.62 mg/mL (1.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.62 mg/mL (1.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.62 mg/mL (1.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 10 mg/mL (20.30 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0302 mL	10.1508 mL	20.3017 mL	50.7542 mL
	5 mM	0.4060 mL	2.0302 mL	4.0603 mL	10.1508 mL
	10 mM	0.2030 mL	1.0151 mL	2.0302 mL	5.0754 mL
	15 mM	0.1353 mL	0.6767 mL	1.3534 mL	3.3836 mL

Keywords

Tepotinib

9 Cited Publications

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Tepotinib

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Publications Citing Use of MedChemExpress (MCE) Tepotinib

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Tepotinib Related Classifications

HY-14721 Related Classifications