Art. -Nr.: HY-50703

MK-2461

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

MK-2461 is an ATP-competitive, selective and orally active wild-type and mutant c-Met inhibitor (IC₅₀s: 0.4-2.5 nM). MK-2461 also inhibits Ron (IC₅₀ of 7 nM) and Flt1 (IC₅₀ of 10 nM), MK-2461 shows selective for c-MET over other kinases (lC₅₀s = 22-7800 nM). MK-2461 can be used for the study of cancer, such as gastric cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.28%
CAS. Nr.: 917879-39-1
Formel: C₂₄H₂₅N₅O₅S
Molecular Weight:495.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MK-2461 Chemical Structure

CAS. Nr.: 917879-39-1

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
GTL 16 cell line	IC₅₀	440 nM Compound: 81, MK-2461	Antiproliferative activity against human GTL16 cells after 72 hrs Antiproliferative activity against human GTL16 cells after 72 hrs	[PMID: 21608528]

In Vitro

MK-2461 (0.61-10000 nM; 2 h) inhibits the phosphorylation of the juxtamembrane domain (Y1003) and the COOH-terminal docking site (Y1349/Y1365) of c-Met and phosphorylation of AKT (S473) and ERK1/2 (T202/Y204)^[1].
MK-2461 is substantially more potent against the autophosphorylation of Y1349 (IC₅₀ of ~100 nM) and Y1365 (IC₅₀ of ~26 nM) in the COOH-terminal docking site than the autophosphorylation of the activation loop (IC₅₀ of ~900 nM)^[1].
MK-2461 potently inhibits the phosphorylation of three nonactivation loop tyrosine residues of c-Met, Y1003 in the juxtamembrane domain and Y1349 and Y1365 in the COOH-terminal docking site (IC₅₀ of ~50 nM). MK-2461 also inhibits the phosphorylation of AKT (S473) and ERK1/2 (T202/Y204). In contrast, MK-2461 has little effect on c-Met activation loop (Y1234/Y1235) phosphorylation^[1].
In the presence of 50 μM ATP (HY-B2176), MK-2461 is equally or more potent against the five mutants (Y1230C, Y1230H, Y1235D, M1250T, and N1100Y) (mean IC₅₀ ranging from 0.4 to 1.5 nM) compared with the wild-type c-Met (mean IC₅₀ = 2.5 nM)^[1].
MK-2461 potently inhibits phosphorylation of the activation loop of FGFR2 (Y653/Y654) and PDGFR-α (Y849) in KATO III cells with IC₅₀ <300 nM^[1].
MK-2461 inhibits HGF-induced mitogenesis of 4MBr-5 monkey lung epithelial cells and HPAF II cells with IC₅₀s of 204 nM and 416 nM, respectively^[1].
MK-2461 potently inhibits IL-3-independent growth of 32D/Tpr-Met and 32D/Tpr-Met (Y362C) cells (IC₅₀ of ~100 nM)^[1].

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

Western Blot Analysis^[1]

Cell Line:

GTL-16 gastric cancer cells
Concentration:

0.61 nM, 2.4 nM, 9.8 nM, 39 nM, 156 nM, 625 nM, 2500 nM, 10000 nM
Incubation Time:

2 h
Result:

Suppressed the phosphorylation of the juxtamembrane domain (Y1003) and the COOH-terminal docking site (Y1349/Y1365) of c-Met and phosphorylation of AKT (S473) and ERK1/2 (T202/Y204) without inhibiting c-Met activation loop (Y1234/35) phosphorylation in GTL-16 gastric cancer cells.

In Vivo

MK-2461 (100 mg/kg; oral gavage; twice daily or once daily; for 21 days) effectively suppresses c-Met signaling and tumor growth in a murine xenograft model of c-Met-dependent gastric cancer^[1].
MK-2461 (134 mg/kg; oral gavage; twice daily; for 21 days) inhibits tumor growth in a model of tumors formed by s.c. injection of mouse NIH-3T3 cells expressing oncogenic c-Met mutants^[1].

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

Animal Model:

Female nude CD-1 nu/nu mice inoculated s.c. with GTL-16 cells to establish c-Met-dependent gastric cancer xenograft model^[1].
Dosage:

10, 50, or 100 mg/kg, 200 mg/kg
Administration:

Oral gavage, twice daily (10, 50, or 100 mg/kg), once daily (200 mg/kg), for 21 days
Result:

At 10, 50, 100 mg/kg, and 200 mg/kg, inhibited tumor growth by 62%, 77%, 75%, and 90%, respectively. Dose-dependent inhibition of phosphorylation of tumor c-Met (Y1349) was observed.

Animal Model:

Female nude CD-1 nu/nu mice inoculated s.c. with mouse NIH-3T3 cells transformed by c-Met single nucleotide mutants T3936C or T3997C^[1].
Dosage:

134 mg/kg
Administration:

Oral gavage, twice daily, for 21 days
Result:

Inhibited growth of T3936C and T3997C tumors by 78% and 62% respectively, and the growth-inhibitory effects were statistically significant.

Clinical Trial

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

Chemical Information

CAS. Nr. 917879-39-1
Appearance Solid
Molecular Weight 495.55
Formel C₂₄H₂₅N₅O₅S
Color Light yellow to yellow
SMILES

O=S(N(C)C[C@H]1OCCOC1)(NC2=CC=C3C=CC(C(C(C3=C2)=O)=C4)=NC=C4C5=CN(N=C5)C)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

All

Sort by:

Journal Impact Factor

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 31 mg/mL (62.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.0180 mL

10.0898 mL

20.1796 mL

5 mM

0.4036 mL

2.0180 mL

4.0359 mL

10 mM

0.2018 mL

1.0090 mL

2.0180 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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)
Handling Instructions (2659 KB)

Verweise

[1]. Pan BS, et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. [Content Brief]

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0180 mL	10.0898 mL	20.1796 mL	50.4489 mL
	5 mM	0.4036 mL	2.0180 mL	4.0359 mL	10.0898 mL
	10 mM	0.2018 mL	1.0090 mL	2.0180 mL	5.0449 mL
	15 mM	0.1345 mL	0.6727 mL	1.3453 mL	3.3633 mL
	20 mM	0.1009 mL	0.5045 mL	1.0090 mL	2.5224 mL
	25 mM	0.0807 mL	0.4036 mL	0.8072 mL	2.0180 mL
	30 mM	0.0673 mL	0.3363 mL	0.6727 mL	1.6816 mL
	40 mM	0.0504 mL	0.2522 mL	0.5045 mL	1.2612 mL
	50 mM	0.0404 mL	0.2018 mL	0.4036 mL	1.0090 mL
	60 mM	0.0336 mL	0.1682 mL	0.3363 mL	0.8408 mL

Keywords

MK-2461

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

MK-2461

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) MK-2461

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MK-2461

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) MK-2461

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MK-2461 Related Classifications

HY-50703 Related Classifications