<Suppliers Price>

MK-2461

Names

[ CAS No. ]:
917879-39-1

[ Name ]:
MK-2461

[Synonym ]:
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)

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]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR
Research Areas >> Cancer

[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.


[Related Small Molecules]

Capmatinib (INCB28060) | Foretinib (GSK1363089) | PHA-665752 | BMS-777607 | Dihexa | Savolitinib | Tivantinib (ARQ 197) | tepotinib | LY2801653 | SGX-523 | DCC-2618 | SU11274 | Ensartinib | CEP-40783 | JNJ-38877605

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℃

Related Compounds