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MK-2461C-Met (WT/mutants) inhibitor

MK-2461

Catalog No. A8476
Size Price Stock Qty
5mg $284.00 In stock
10mg $498.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

MK-2461

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

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Chemical Properties

Cas No. 917879-39-1 SDF Download SDF
Chemical Name 9-[[[(2R)-1,4-dioxan-2-yl]methyl-methylsulfamoyl]amino]-2-(1-methylpyrazol-4-yl)-11-oxobenzo[1,2]cyclohepta[2,4-b]pyridine
Canonical SMILES CN1C=C(C=N1)C2=CN=C3C=CC4=C(C=C(C=C4)NS(=O)(=O)N(C)CC5COCCO5)C(=O)C3=C2
Formula C24H25N5O5S M.Wt 495.55
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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.