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MK-2461

Catalog No. T6094 CAS 917879-39-1

Synonyms: MK2461

MK-2461 is a novel inhibitor that targets multiple proteins and competitively binds to ATP sites, specifically inhibiting the activated c-Met protein with an average inhibitory concentration (IC50) of 2.5 nM.

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MK-2461, CAS 917879-39-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 77.00
5 mg	In stock	$ 150.00
10 mg	In stock	$ 263.00
25 mg	In stock	$ 531.00
50 mg	In stock	$ 768.00
100 mg	In stock	$ 1,070.00
500 mg	In stock	$ 2,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 162.00

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Purity: 99.53%

ee: 100%

Purity: 98.36%

Purity: 95.41%

Biological Description

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Description	MK-2461 is a novel inhibitor that targets multiple proteins and competitively binds to ATP sites, specifically inhibiting the activated c-Met protein with an average inhibitory concentration (IC50) of 2.5 nM.
Targets&IC50	c-Met:2.5 nM
In vitro	MK-2461 also potently inhibits FGFR1, FGFR2, FGFR3, KDR, TrkA, TrkB, and Flt4 with IC50 of 65 nM, 39 nM, 50 nM, 44 nM, 46 nM, 61 nM, and 78 nM, respectively. Compared with wild-type c-Met, MK-2461 more potently inhibits the activity of oncogenic c-Met kinase mutants such as N1100Y, Y1230C, Y1230H, Y1235D, and M1250T with IC50 of 1.5 nM, 1.5 nM, 1.0 nM, 0.5 nM, and 0.4 nM, respectively. MK-2461 binds more strongly to phosphorylated c-Met than to unphosphorylated c-Met. MK-2461 potently inhibits ATP-induced autophosphorylation of the COOH-terminal docking domain of c-Met, but not the activation loop. In contrast, MK-2461 inhibits phosphorylation of the activation loop of FGFR2 (Y653/Y654) in Kato III cells and PDGFRα (Y849) in H1703 cells with IC50 of <0.3 μM. MK-2461 inhibits HGF-induced mitogenesis of 4MBr-5 cells with IC50 of 204 nM, and HGF-induced migration of HPAF II cells with IC50 of 404 nM, as well as HGF-induced branching tubulogenesis of MDCK cells. In addition, MK-2461 potently inhibits IL-3-independent proliferation of 32D cells transformed with Tpr-Met or Tpr-Met (Y362C) mutant with IC50 of ~100 nM. MK-2461 significantly inhibits the proliferation of a large panel of tumor cell lines, especially potent against tumor cells harbored genomic amplification of MET or FGFR2. [1]
In vivo	MK-2461 treatment significantly inhibits c-Met (Y1349) phosphorylation in GTL-16 tumors with IC50 of ~1 μM. Oral administration of MK-2461 at 10 mg/kg, 50 mg/kg, and 100 mg/kg twice daily as well as 200 mg/kg once daily effectively suppresses tumor growth of GTL-16 xenografts in mice by 62%, 77%, 75%, and 90%, respectively. Similarly, MK-2461 treatment at 134 mg/kg twice daily inhibits the growth of NIH3T3 tumors harboring c-Met single nucleotide mutants T3936C and T3997C, by 78% and 62%, respectively. [1]
Kinase Assay	Time-resolved fluorescence resonance energy transfer assay: The c-Met–catalyzed phosphorylation of N-biotinylated peptide (EQEDEPEGDYFEWLE-CONH2) is measured using a time-resolved fluorescence resonance energy transfer assay. [2] The MK-2461 IC50 for Ron, Mer, Flt1, Flt3, Flt4, KDR, PDGFRβ, FGFR1, FGFR2, FGFR3, TrkA, and TrkB are determined using time-resolved fluorescence resonance energy transfer assays similar to the c-Met kinase assay.
Cell Research	Cells are exposed to various concentrations of MK-2461 for 72 hours. The viability of tumor cells is measured using the ViaLight PLUS kit.(Only for Reference)

Synonyms	MK2461
Molecular Weight	495.55
Formula	C24H25N5O5S
CAS No.	917879-39-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 92 mg/mL (185.7 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Pan BS, et al. Cancer Res, 2010, 70(4), 1524-1533. 2. Park YW, et al. Anal Biochem, 1999, 269(1), 94-104.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Bioactive Compound Library Bioactive Compounds Library Max Clinical Compound Library

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Tepotinib Cabozantinib hydrochloride SGI-7079 MK-8033 c-Met-IN-2 Capmatinib 2HCl.H2O PF-04217903 methanesulfonate NPS-1034

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Keywords

MK-2461 917879-39-1 Tyrosine Kinase/Adaptors c-Met/HGFR MK2461 inhibit Inhibitor MK 2461 inhibitor

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