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MK-2461

Catalog No.
A8476
C-Met (WT/mutants) inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$205.00
In stock
5mg
$189.00
In stock
10mg
$330.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

MK-2461 is a potent inhibitor of Met, Flt1, Flt 3, Ron, PDGFRβ, and Mer with IC50 of 2.5 nM, 10 nM, 22 nM, 7 nM, and 24 nM, respectively.

c-Met, also named as hepatocyte growth factor receptor (HGFR) is a receptor tyrosine kinase that is essential for embryonic development and would healing. In many tumor cells, this molecular is overexpressed or mutated and was found to play important roles in tumor cell proliferation, survival, invasion, metastasis and angiogenesis.

In vitro, MK-2461treatment blocked hepatocyte growth factor/c-Met- dependent mitogenesis, migration, cell scatter, and tubulogenesis 1.

In a murine xenograft model of c-Met-dependent gastric cancer, oral administration of MK-2461 at a dosge of 100 mg/kg twice daily effectively inhibited c-Met signaling and tumor growth 1. Consistently, MK-2461 inhibited the tumor growth which was formed by s.c. injection of mouse NIH-3T3 cells expressing oncogenic c-Met mutants 1. These evidence support the preclinical development of MK-2461 for cancer therapy.

Reference:
1.   Pan BS, Chan GK, Chenard M, et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer research. 2010;70(4):1524-1533.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt495.55
Cas No.917879-39-1
FormulaC24H25N5O5S
Solubility≥24.8 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
Chemical Name9-[[[(2R)-1,4-dioxan-2-yl]methyl-methylsulfamoyl]amino]-2-(1-methylpyrazol-4-yl)-11-oxobenzo[1,2]cyclohepta[2,4-b]pyridine
SDFDownload SDF
Canonical SMILESCN1C=C(C=N1)C2=CN=C3C=CC4=C(C=C(C=C4)NS(=O)(=O)N(C)CC5COCCO5)C(=O)C3=C2
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description MK-2461 is a potent, multi-targeted inhibitor of c-Met(WT/mutants) with IC50 values of 0.4-2.5 nM.
Targets c-Met (M1250T) c-Met (Y1235D) c-Met (Y1230H) c-Met (N1100) c-Met (Y1230C c-Met
IC50 0.4 nM 0.5 nM 1.0 nM 1.5 nM 1.5 nM 2.5 nM

Quality Control

Quality Control & MSDS

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Chemical structure

MK-2461