MK-2461
Product Specifications
UNSPSC 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-Met
in 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]
Target Antigen
c-Met/HGFR
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/MK-2461.html
Purity
99.61
Solubility
DMSO : ≥ 31 mg/mL
Smiles
O=S(N(C)C[C@H]1OCCOC1)(NC2=CC=C3C=CC(C(C(C3=C2)=O)=C4)=NC=C4C5=CN(N=C5)C)=O
Molecular Weight
495.5508
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-50703/MK-2461-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-50703/MK-2461-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
917879-39-1
Available Sizes
Curated Selection
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