MK-2461

MK-2461

• CAS Number: 917879-39-1
• 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)
• Clinical Information: Phase 2