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1H NMR (600 MHz, DMSO-d6) δ 9.21 (d, 1H), 8.53 (d, 1H), 8.47 (m, 1H), 8.46 (m, 1H), 8.15 (d, 1H), 8.14 (s, 1H), 7.78 (m, 4H), 7.39 (m, 2H), 7.32 (d, 1H), 7.24 (m, 1H), 4.63 (s, 2H), 4.22 (d, 1H), 3.88 (s, 3H).
Kinase selectivity @ 1 μmol/L was tested using 221 kinases by Millipore and only c-Met and Ron, were inhibited by more than 90%, 4 other kinases (Fes, FGFR3, Flt4, Mer) were inhibited by more than 50%, with the inhibition ranging from 60 to 70%. Titration experiments demonstrated that MK-8033 is >100-fold selective relative to Ron and c-Met inhibition versus the measured kinome.
Mutant Potency (nM): c-Met 1.3 WT, 2.0 N1100Y, 1.0 Y1230C, 0.6 Y1230H, 0.6 Y1235D, 1.2 M1250T
Outside target family: weak inhibitor of cytochrome P450s at high μM concentrations (IC50s > 11 μM)