Table 2. Key Properties of BRD2879.
in vitro enzyme inhibition, IC50a | |
---|---|
IDH1-R132H | 0.05 μM |
IDH1-R132C | 2.5 μM |
IDH1-WT | >20 μM |
IDH2-R140Q | >20 μM |
thermal stabilizationb | |
---|---|
IDH1-R132H | 3.7 °C |
IDH1-R132C | 1.4 °C |
cell-based R-2HG suppression, EC50c | |
---|---|
HA1E-M-IDH1-R132H | 0.3 μM |
mechanism of inhibition | |
---|---|
w.r.t. α-KG | competitive |
w.r.t. Mg2+ | competitive |
microsomal stability, t1/2f | |
---|---|
mouse | 0.7 min |
human | 0.7 min |
plasma protein bindingd | |
---|---|
mouse | 96.3% |
human | 99.5% |
Geometric mean of at least three independent experiments.
Mean of three independent experiments, each with seven replicates.
Mean of three independent experiments, each with three replicates.
Mean of three replicates in one experiment.
Single experiment, includes 1% DMSO.
Single experiment, calculated from a 6-point curve over 1 h.