DC Chemicals · Product datasheet

Pinometostat(EPZ5676) — Datasheet

CAT. NO. DC4242

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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.

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