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EPZ011989

Cat. No. M8933
EPZ011989 Structure
Size Price Availability Quantity
10mg USD 150 In stock
25mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
Cell Experiment
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
Animal models SCID mice
Formulation 0.5% methyl cellulose and 0.1% Tween-80
Dosages 250 and 500 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 605.81
Formula C35H51N5O4
CAS Number 1598383-40-4
Purity >98%
Solubility DMSO: ≥ 10 mg/mL
Storage at -20°C
References

EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.
Campbell JE, et al. ACS Med Chem Lett. 2015 Mar 4;6(5):491-5. PMID: 26005520.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: EPZ011989 supplier, Histone Methyltransferase, inhibitors

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