Mk-2461 .

ChemicalBook > CAS DataBase List > 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 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;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]-;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;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
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)

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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-2206 2HCl MK-4101 mk-1064 MK 0557 MK-5172 (E)-3-[[[3-[2-(7-CHLORO-2-QUINOLINYL)ETHENYL]PHENYL]-[[(3-DIMETHYLAMINO)-3-OXOPROPYL]THIO]METHYL]THIO]-PROPANOIC ACID, SODIUM SALT Omarigliptin (MK-3102) N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide ABT 737 SU 11274 Ruxolitinib Olaparib Sitafloxacin Sesquihydrate MK-8998 MK-1775 SCH900776 MK-0752

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

917879-39-1

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