MK-2461

A selective c-MET inhibitor
Catalog #: B3359 | abID:

Product Details

Alternate Name MK2461 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
Appearance Solid
CAS # 917879-39-1
Molecular Formula C₂₄H₂₅N₅O₅S
Molecular Weight 495.55
Purity ≥98% by HPLC
Solubility >50 mg/ml DMSO
SMILES CN1C=C(C=N1)C2=CC3=C(C=CC4=C(C3=O)C=C(C=C4)NS(=O)(=O)N(C)CC5COCCO5)N=C2
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/t20-/m1/s1
InChi Key JGEBLDKNWBUGRZ-HXUWFJFHSA-N
PubChem CID 44137946
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20ºC
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met. MK-2461 inhibits in vitro phosphorylation of a peptide substrate recognized by wild-type or oncogenic c-Met kinases (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC50 values of 0.4 to 2.5 nmol/L. In contrast, MK-2461 was several hundredfold less potent as an inhibitor of c-Met autophosphorylation at the kinase activation loop.


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