POMHEX
目录号: PL11771 纯度: ≥99%
CAS No. :2004714-34-3
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中文名称
POMHEX
英文名称
POMHEX
英文别名
POMHEX
Cas No.
2004714-34-3
分子式
C17H32NO9P
分子量
425.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
POMHEX 是一个消旋混合物,是具有细胞渗透性的 HEX 的 POM 前体药物,是 ENO2 的特异性抑制剂。POMHEX 对 ENO1 缺失的细胞表现出低纳摩尔级别活性,并对 ENO1 缺失的肿瘤模型表现出良好的抗癌效果。POMHEX 是有效的糖酵解抑制剂。
生物活性
POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor.
性状
Solid
体外研究(In Vitro)
POMHEX (78 nM, 8h) minimally impacts ENO1-WT glioma cells but profoundly affected ENO1-deleted cells.
POMHEX (0-720 nM) selectively induces energy stress, inhibits proliferation and triggers apoptosis in ENO1-deleted glioma cells.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
POMHEX (i.v., ip) injections are consistently tolerated without haemolytic anaemia at doses of up to 10 mg per kg (body weight) per day. POMHEX (i.v., 35 mg/kg) results in lethargy that prompted veterinarians to perform euthanasia.
POMHEX is rapidly hydrolysed to HemiPOMHEX in mouse plasma ex vivo, with a half-life of approximately 30 s, the half-life in human blood ex vivo was about 9min.
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
参考文献
[1]. Yu-Hsi Lin, et al. An enolase inhibitor for the targeted treatment of ENO1-deleted cancers. Nat Metab. 2020 Nov 23.
溶解度数据
In Vitro: DMSO : 100 mg/mL (236.18 mM; Need ultrasonic)配制储备液
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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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