E3330 (Synonyms: APX-3330)
目录号: PL04875 纯度: ≥99%
CAS No. :136164-66-4
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中文名称
E3330
中文别名
E3330 抑制剂
英文名称
E3330
英文别名
(2E)-2-[(4,5-dimethoxy-2-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl)methylidene]undecanoic acid;E 3330;(2E)-2-[(4,5-Dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid;E3330;APX-3330
Cas No.
136164-66-4
分子式
C21H30O6
分子量
378.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
E3330 (APX-3330) 是一种直接,口服有效的,选择性的 Ape-1 (无嘌呤/嘧啶内切酶 1)/Ref-1 (氧化还原因子 -1) 氧化还原的抑制剂。E3330 能抑制胰腺癌组织中 NF-κB、AP-1、HIF-1α 的活性。E3330 具有抗癌活性。
生物活性
E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.
性状
Solid
IC50 & Target[1][2]
Ape-1, Ref-1
体外研究(In Vitro)
E3330 (0-50 μM, 48 h) inhibits the growth of HUVECs, PCECs and EPCs.
E3330 (0-5 μM) reduces secreted and intracellular VEGF (vascular endothelial growth factor) expression by pancreatic cancer cells, while concomitantly downregulating the cognate receptor Flk-1/KDR on PCECs.
E3330 (0-1 μM) inhibits the differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into CD31 cells of endothelial lineage.
E3330 (0-50 μM, 72 h) decreases cell viability in H1975 cells about 45% at 50 μM.
E3330 (0-30 μM) inhibits the growth and migration of pancreatic cancer cells.
E3330 (0-30 μM) significantly enhances intracellular ROS level and inhibits CD44 expression in PANC1 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
E3330 (25 mg/kg, Orally, 5 daily, five days each week for three weeks) is neuroprotective against cisplatin-induced alterations in capsaicin-induced vasodilation.
E3330 (0-100 mg/kg, Orally, once) attenuates the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge. 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]. Zou GM, et al. The Ape-1/Ref-1 redox antagonist E3330 inhibits the growth of tumor endothelium and endothelial progenitor cells: therapeutic implications in tumor angiogenesis. J Cell Physiol. 2009 Apr;219(1):209-18.
[2]. Manguinhas R, et al. Impact of the APE1 Redox Function Inhibitor E3330 in Non-small Cell Lung Cancer Cells Exposed to Cisplatin: Increased Cytotoxicity and Impairment of Cell Migration and Invasion. Antioxidants (Basel). 2020 Jun 24;9(6):550.
溶解度数据
In Vitro: DMSO : 120 mg/mL (317.07 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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