EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
Cell Experiment | |
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Cell lines | WSU-DLCL2 cells |
Preparation method | For assessment of cell proliferation and viability, exponentially growing cells are plated, in triplicate, in 96-well plates. Cells are incubated with increasing concentrations of EPZ011989. Viable cell number is determined every 3-4 days for up to 11 days using the Guava Viacount assay. |
Concentrations | 0-10 μM |
Incubation time | 0-11 days |
Animal Experiment | |
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Animal models | SCID mice |
Formulation | 0.5% methyl cellulose and 0.1% Tween-80 |
Dosages | 250 and 500 mg/kg |
Administration | p.o. |
Molecular Weight | 605.81 |
Formula | C35H51N5O4 |
CAS Number | 1598383-40-4 |
Solubility (25°C) | DMSO: ≥ 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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