Table 1.

IC50 values for methylation and proliferation as well as LCC values for EPZ-6438 in human lymphoma cell lines

Cell lineEZH2 statusMethylation IC50 (nmol/L)aProliferation IC50 (μmol/L)bLCC (μmol/L)b
DOHH-2Wild-type31.7>10
FarageWild-type20.099>10
OCI-LY19Wild-type86.2>10
ToledoWild-typeND7.6>10
KARPAS-422Y646N900.00180.12
PfeifferA682G20.000490.0005
RLY646N225.8>10
SU-DHL-10Y646FND0.00580.14
SU-DHL-6Y646N200.00470.21
WSU-DLCL2Y646F90.00860.17

Abbreviation: ND, not determined.

  • aDerived after incubation for 4 days by immunoblot. Values represent the result from 1 experiment.

  • bDerived after incubation for 11 days. Compound incubations for each experiment were performed in triplicate, and values represent 1 experiment for all cell lines except OCI-LY19, Pfeiffer, and WSU-DLCL2. For the remaining 3 cell lines, values represent the mean from the following number of experiments: OCI-LY19, n = 9; Pfeiffer, n = 2; and WSU-DLCL2, n = 15.