Structure information available on request
Chemical structureResearch use only
CAT. NO. DC4242Featured

Pinometostat(EPZ5676)

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Product overview

Description & Application

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

ParameterValue
Chemical NamePinometostat
CAS No.1380288-87-8
SynonymsEPZ-5676;(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-(((3-(2-(6-tert-butyl-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)-tetrahydrofuran-3,4-diol;(2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol;9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofura...;9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine;EPZ 5676;Pinometostat (EPZ5676);5'-[{cis-3-[2-(5-Tert-Butyl-1h-Benzimidazol-2-Yl)ethyl]cyclobutyl}(Propan-2-Yl)amino]-5'-Deoxyadenosine;CS-1419;EP6;Pinometostat;S7062,EPZ5676;EPZ5676;8V9YR09EF3;F66X4M38G5;(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol;Pinometostat, trans-;(2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-(((3-(2
FormulaC30H42N8O3
M.Wt562.7063
SMILESO1[C@]([H])([C@@]([H])([C@@]([H])([C@@]1([H])C([H])([H])N(C([H])(C([H])([H])[H])C([H])([H])[H])C1([H])C([H])([H])C([H])(C([H])([H])C([H])([H])C2=NC3C([H])=C([H])C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=C([H])C=3N2[H])C1([H])[H])O[H])O[H])N1C([H]
Purity99%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

In Vitro

Pinometostat (EPZ-5676) inhibits H3K79me2 with IC50 values of 3 nM and 5 nM in MV4-11 and HL60 cells, respectively. Pinometostat (EPZ-5676) is a potent inhibitor of MV4-11 proliferation with an IC50 value of 3.5 nM[1]. Pinometostat (EPZ-5676) induces a synergistic and durable antiproliferative effect, increases expression of differentiation markers and apoptosis as dingle agent, and demonstrates combination benefit in combination with AML standard of care drugs in MLL-r cells[2].

In Vivo

Pinometostat (EPZ-5676) (70 mg/kg, i.p.) causes complete and sustained regression in a rat xenograft model of MLL-rearranged leukemia. Pinometostat (EPZ-5676) (70, 35 mg/kg, i.v.) reduces HOXA9 and MEIS1 mRNA levels of tumors taken from rats, and reduces MLL-fusion target gene expression in vivo[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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