Tepotinib (Synonyms: EMD-1214063)

Name: Tepotinib
Brand: MedChemExpress
SKU: HY-14721
Rating: 5.0 (6 reviews)

製品番号: HY-14721 純度: 99.94%: Data Sheet SDS COA 取扱説明書
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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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CAS 番号 : 1100598-32-0

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 103	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 103	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$95	在庫あり	Estimated Time of Arrival: December 31
10 mg	$150	在庫あり	Estimated Time of Arrival: December 31
25 mg	$300	在庫あり	Estimated Time of Arrival: December 31
50 mg	$420	在庫あり	Estimated Time of Arrival: December 31
100 mg	$550	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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Based on 6 publication(s) in Google Scholar

Other Forms of Tepotinib:

Tepotinib (Standard) 在庫あり
Tepotinib hydrochloride お問い合わせ

顧客検証

: 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.

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製品説明

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]

体外実験

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.

体内実験

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.

臨床実験

分子量

492.57

分子式

C₂₉H₂₈N₆O₂

CAS 番号

1100598-32-0

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.

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

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.94%

Select Batch:

データシート (275 KB) SDS (393 KB)

COA (244 KB) HNMR (273 KB) LCMS (93 KB)

取扱説明書 (2659 KB)

参考文献

[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.

Complete Stock Solution Preparation Table

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

Tepotinib Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tepotinib1100598-32-0EMD-1214063EMD1214063EMD 1214063c-Met/HGFRAutophagyInhibitorinhibitorinhibit

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Tepotinib (Synonyms: EMD-1214063)

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Other Forms of Tepotinib:

Tepotinib 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Tepotinib 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tepotinib Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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