MK-2461

Modify Date: 2024-01-11 16:42:23

MK-2461 Structure
MK-2461 structure
Common Name MK-2461
CAS Number 917879-39-1 Molecular Weight 495.551
Density 1.5±0.1 g/cm3 Boiling Point 732.4±70.0 °C at 760 mmHg
Molecular Formula C24H25N5O5S Melting Point N/A
MSDS N/A Flash Point 396.7±35.7 °C

 Use of MK-2461


MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: c-Metin vitro: MK-2461 inhibits the kinase activity of human c-Met with a mean IC50 of 2.5 nM in the presence of 50 μM ATP. Ron (IC50 = 7 nM) and Flt1 (IC50 = 10 nM) are inhibited by MK-2461 with similar potencies to c-Met (IC50 = 2.5 nM), whereas nine other kinases, including FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB, are found to be 8- to 30-fold less sensitive to MK-2461 than c-Met. [1]in vivo: MK-2461 inhibits c-Met signaling and tumor growth in tumor xenograft models in mice.[1]

 Names

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
Synonym More Synonyms

 MK-2461 Biological Activity

Description MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.IC50 value: 2.5 nM [1]Target: c-Metin vitro: MK-2461 inhibits the kinase activity of human c-Met with a mean IC50 of 2.5 nM in the presence of 50 μM ATP. Ron (IC50 = 7 nM) and Flt1 (IC50 = 10 nM) are inhibited by MK-2461 with similar potencies to c-Met (IC50 = 2.5 nM), whereas nine other kinases, including FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB, are found to be 8- to 30-fold less sensitive to MK-2461 than c-Met. [1]in vivo: MK-2461 inhibits c-Met signaling and tumor growth in tumor xenograft models in mice.[1]
Related Catalog
References

[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.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 732.4±70.0 °C at 760 mmHg
Molecular Formula C24H25N5O5S
Molecular Weight 495.551
Flash Point 396.7±35.7 °C
Exact Mass 495.157654
PSA 124.03000
LogP -0.52
Vapour Pressure 0.0±2.4 mmHg at 25°C
Index of Refraction 1.693
Storage condition -20℃

 Synonyms

Sulfamide, N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N'-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-
MK-2461
cc-600
UNII-4200RD53XF
N-[(2R)-1,4-Dioxan-2-ylmethyl]-N-methyl-N'-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfuric diamide
Sulfamide,N-((2R)-1,4-dioxan-2-ylmethyl)-N-methyl-N'-(3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo(4,5)cyclohepta(1,2-b)pyridin-7-yl)
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