Pinometostat (EPZ-5676) demonstrates inhibition of H3K79me2, showing IC50 values of 3 nM in MV4-11 cells and 5 nM in HL60 cells. It effectively suppresses MV4-11 cell growth with an IC50 of 3.5 nM[1]. Pinometostat shows a potent, synergistic, and lasting suppressive effect on cell growth, enhances markers of differentiation and apoptosis, and yields additional benefits when used with standard AML treatments in MLL-r cell types[2].
体内研究
With an intraperitoneal dose of 70 mg/kg, Pinometostat leads to a full and enduring regression in a rat model of MLL-rearranged leukemia. Intravenous doses of 70 and 35 mg/kg reduce HOXA9 and MEIS1 mRNA levels in tumors from rats and diminish MLL-fusion target gene expression in live subjects[1].
体外研究
Pinometostat (EPZ-5676) demonstrates inhibition of H3K79me2, showing IC50 values of 3 nM in MV4-11 cells and 5 nM in HL60 cells. It effectively suppresses MV4-11 cell growth with an IC50 of 3.5 nM[1].
Pinometostat shows a potent, synergistic, and lasting suppressive effect on cell growth, enhances markers of differentiation and apoptosis, and yields additional benefits when used with standard AML treatments in MLL-r cell types[2].
作用机制
EPZ-5676 occupies the SAM binding pocket and induces conformational changes in DOT1L[1].
Pinometostat 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
human MOLM13 cells
Proliferation assay
Antiproliferative activity against human MOLM13 cells containing MLL-AF9, EC50=4 nM
23879463
human MV4-11 cells
Function assay
4 days
Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA method
25406853
human MV4-11 cells
Proliferation assay
Antiproliferative activity against human MV4-11 cells containing MLL-AF4, EC50=4 nM
23879463
human THP1 cells
Proliferation assay
Antiproliferative activity against human THP1 cells containing MLL-AF9, EC50=4 nM
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