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Pinometostat

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Chemical Structure| 1380288-87-8 同义名 : EPZ-5676
CAS号 : 1380288-87-8
货号 : A228248
分子式 : C30H42N8O3
纯度 : 99%+
分子量 : 562.706
MDL号 : MFCD24849416
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(186.6 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(177.71 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • Histone Methyltransferase

    DOT1L, Ki:80 pM
描述 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].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.89mL

1.78mL

0.89mL

17.77mL

3.55mL

1.78mL
参考文献

[1]Daigle SR, et al. Potent inhibition of DOT1L as treatment for MLL-fusion leukemia. Blood. 2013 Jun 25. [Epub ahead of print]

[2]Klaus CR, et al. DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells. J Pharmacol Exp Ther. 2014 Sep;350(3):646-56.