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Pinometostat (EPZ5676)

Pinometostat (EPZ5676) 1380288-87-8
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Chemical Information
Product name:Pinometostat (EPZ5676) Purity:98%min
CAS NO:1380288-87-8 Solubility:Soluble in DMSO
Molecular Formula:C30H42N8O3 Package:Packaging according to customer requirements
Molecular Weight:562.71 Storage:Store at -20℃
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Remarks

Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.

EPZ-5676 inhibits H3K79me2 with IC50 values of 3 nM and 5 nM in MV4-11 and HL60 cells, respectively. EPZ-5676 is a potent inhibitor of MV4-11 proliferation with an IC50 value of 3.5 nM[1]. 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].

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