ChemicalBook > CAS DataBase List > Mk-2461 .

Mk-2461 .

Product Name
Mk-2461 .
CAS No.
917879-39-1
Chemical Name
Mk-2461 .
Synonyms
CS-528;Mk-2461 .;Mk-2461 USP/EP/BP;MK-2461;MK2461;MK 2461;MK-2461, 10 mM in DMSO;MK-2461 c-Met HGFR Inhibitor;9-[[[(2R)-1,4-DIOXAN-2-YL]METHYL-METHYLSULFAMOYL]AMINO]-2-(1-METHYLPYRAZOL-4-YL)-11-OXOBENZO[1,2]CYCLOHEPTA[2,4-B]PYRIDINE;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]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]sulfamide;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]-
CBNumber
CB22123242
Molecular Formula
C24H25N5O5S
Formula Weight
495.55
MOL File
917879-39-1.mol
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Mk-2461 . Property

Melting point:
192-193 °C
Boiling point:
732.4±70.0 °C(Predicted)
Density 
1.45±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≥24.8 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form 
solid
pka
6.81±0.20(Predicted)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
M425035
Product name
MK-2461
Packaging
1mg
Price
$160
Updated
2021/12/16
ChemScene
Product number
CS-5537
Product name
MK-2461
Purity
99.92%
Packaging
5mg
Price
$180
Updated
2021/12/16
ApexBio Technology
Product number
A8476
Product name
MK-2461
Packaging
5mg
Price
$189
Updated
2021/12/16
ApexBio Technology
Product number
A8476
Product name
MK-2461
Packaging
10mM(in 1mL DMSO)
Price
$205
Updated
2021/12/16
ChemScene
Product number
CS-5537
Product name
MK-2461
Purity
99.92%
Packaging
10mg
Price
$320
Updated
2021/12/16
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Mk-2461 . Chemical Properties,Usage,Production

Uses

MK-2461 is a potent inhibitor of c-Met, Ron, Flt1/3, PDGFRβ, Mer and FGFR1/2/3 with IC50 of 2.5 nM, 7 nM, 10 nM/22 nM, 22 nM, 24 nM and 65 nM/39 nM/50 nM, respectively.

Uses

MK-2461 is a novel ATP-competitive multitargeted kinase inhibitor that preferentially inhibits the activated c-Met receptor. MK-2461 is also a potent inhibitor of Ron, Flt1, Flt 3, PDGFRβ, and Mer receptors. Recent studies show that MK-2461 siginifciantly suppresses tumor growth of GTL-16 xenografts in mice and MK-2461 treatments effectively inhibit the growth of NIH3T3 tumors harboring c-Met single nucleotide mutants T3936C and T3997C.

Biological Activity

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 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.

in vitro

mk-2461treatment blocked hepatocyte growth factor/c-met- dependent mitogenesis, migration, cell scatter, and tubulogenesis 1.

target

c-Met (M1250T)

References

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.

Mk-2461 . Preparation Products And Raw materials

Raw materials

Preparation Products

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Mk-2461 . Suppliers

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917879-39-1, Mk-2461 .Related Search:


  • Mk-2461 .
  • N-[(2R)-1,4-dioxan-2-ylMethyl]-N-Methyl{[5-(1-Methyl-1H-pyrazol-4-yl)-2-oxo-7-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-14-yl]aMino}sulfonaMide
  • 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]sulfamide
  • Mk-2461 . N-[(2R)-1,4-dioxan-2-ylMethyl]-N-Methyl{[5-(1-Methyl-1H-pyrazol-4-yl)-2-oxo-7-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-14-yl]aMino}sulfonaMide
  • 9-[[[(2R)-1,4-DIOXAN-2-YL]METHYL-METHYLSULFAMOYL]AMINO]-2-(1-METHYLPYRAZOL-4-YL)-11-OXOBENZO[1,2]CYCLOHEPTA[2,4-B]PYRIDINE
  • MK-2461;MK2461;MK 2461
  • CS-528
  • 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 USP/EP/BP
  • MK-2461 c-Met HGFR Inhibitor
  • 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]sulfamide
  • MK-2461, 10 mM in DMSO
  • 917879-39-1
  • Inhibitors
  • Aromatics
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  • Tyrosine Kinase Inhibitors