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 Target: c-Metin 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. in vivo: MK-2461 inhibits c-Met signaling and tumor growth in tumor xenograft models in mice.
Product information
CAS Number: 917879-39-1
Molecular Weight: 495.55
Formula: C24H25N5O5S
Chemical Name: 14-({[(1,4-dioxan-2-yl)methyl](methyl)sulfamoyl}amino)-5-(1-methyl-1H-pyrazol-4-yl)-7-azatricyclo[9.4.0.0³,⁸]pentadeca-1(11),3,5,7,9,12,14-heptaen-2-one
Smiles: CN(CC1COCCO1)S(=O)(=O)NC1=CC2=C(C=CC3=NC=C(C=C3C2=O)C2=CN(C)N=C2)C=C1
InChiKey: JGEBLDKNWBUGRZ-UHFFFAOYSA-N
InChi: InChI=1S/C24H25N5O5S/c1-28-13-18(12-26-28)17-9-22-23(25-11-17)6-4-16-3-5-19(10-21(16)24(22)30)27-35(31,32)29(2)14-20-15-33-7-8-34-20/h3-6,9-13,20,27H,7-8,14-15H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 31 mg/mL (62.56 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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