Pinometostat|1380288-87-8|(EPZ-5676)-陌孚医药/Medlife

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Pinometostat (Synonyms: EPZ-5676)

目录号: PL15064 纯度: ≥99%

CAS No. :1380288-87-8

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中文名称	Pinometostat
中文别名	2,3-二氢-1-(3-羟基丙基)-5-[(2R)-2-[[2-[2-(2,2,2-三氟乙氧基)苯氧基]乙基]氨基]丙基]-1H-吲哚-7-甲腈;9-[5-脱氧-5-[[顺式-3-[2-[6-(1,1-二甲基乙基)-1H-苯并咪唑-2-基]乙基]环丁基](1-甲基乙基)氨基]-β-D-呋喃核糖]-9H-嘌呤-6-胺;9-[5-脱氧-5-[[顺式-3-[2-[6-叔丁基-1H-苯并咪唑-2-基]乙基]环丁基](1-甲基乙基)氨基]-BETA-D-呋喃核糖基]-9H-嘌呤-6-胺;EPZ5676 抑制剂
英文名称	Pinometostat
英文别名	EPZ-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
Cas No.	1380288-87-8
分子式	C₃₀H₄₂N₈O₃
分子量	562.71
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Pinometostat (EPZ-5676) 是有效的DOT1L组蛋白甲基转移酶抑制剂， K_i 为 80 pM。

生物活性

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

性状

Solid

IC50 & Target[1][2]

Ki: < 80 pM (DOT1L histone methyltransferase)

体外研究(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. Pinometostat (EPZ-5676) induces a synergistic and durable antiproliferative effect, increases expression of differentiation markers and apoptosis as single agent, and demonstrates combination benefit in combination with AML standard of care drugs in MLL-r cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (177.71 mM; Need ultrasonic)Ethanol : 100 mg/mL (177.71 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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