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MK-2461 - 10mM in DMSO, high purity , CAS No.917879-39-1(DMSO), Hepatocyte growth factor receptor inhibitor

COA COA
In stock
Item Number
M408922
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SKU Size
Availability
 Price Qty
M408922-1ml
1ml
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$587.90
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FGFR1 Selective Inhibitors

View related series
Compound libraries (12325)

Basic Description

Synonyms 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
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Hepatocyte growth factor receptor inhibitor
Product Description

Information

MK-2461 is a potent, multi-targeted inhibitor forc-Met(WT/mutants)withIC50of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2.
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.

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.
Cell Data

cell lines：A2780 human ovarian cell line

Concentrations：Dissolved in DMSO, final concentrations ~100 μM

Incubation Time：72 hours

Powder Purity:≥99%

Product Properties

ALogP 0.924
hba_count 7
HBD Count 1
Rotatable Bond 6

Associated Targets(Human)

MST1R Tchem Macrophage-stimulating protein receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT4 Tclin Vascular endothelial growth factor receptor 3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FGFR1 Tclin Fibroblast growth factor receptor 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FGFR2 Tclin Fibroblast growth factor receptor 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FGFR3 Tclin Fibroblast growth factor receptor 3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MET Tclin Hepatocyte growth factor receptor (15 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MERTK Tchem Tyrosine-protein kinase Mer (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PDGFRB Tclin Platelet-derived growth factor receptor beta (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT1 Tclin Vascular endothelial growth factor receptor 1 (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK2 Tclin BDNF/NT-3 growth factors receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK1 Tclin High affinity nerve growth factor receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles CN(CC1COCCO1)[S](=O)(=O)NC2=CC3=C(C=C2)C=CC4=C(C=C(C=N4)C5=C[N](C)N=C5)C3=O
Molecular Weight 495.55
Reaxy-Rn 12752051
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12752051&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 13 mg/mL (52.26 mM); Water: 13 mg/mL (52.26 mM); Ethanol: 13 mg/mL (52.26 mM);
DMSO(mg / mL) Max Solubility 99
DMSO(mM) Max Solubility 199.78
Water(mg / mL) Max Solubility <1

Solution Calculators

Reviews

Customer Reviews

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