生物活性 | E3330 (APX-3330) is a direct, orally active and selective inhibitor ofApe-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1)redox. E3330 is able to impair tumor growth and blocks the activity ofNF-κB,AP-1, andHIF-1αin pancreaticcancer. E3330 shows anticancer activities[1][2][3][4][5]. |
IC50& Target | |
体外研究 (In Vitro) | E3330 (0-50 μM, 48 h) inhibits the growth of HUVECs, PCECs and EPCs[1]. 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[1]. E3330 (0-1 μM) inhibits the differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into CD31+cells of endothelial lineage[1]. E3330 (0-50 μM, 72 h) decreases cell viability in H1975 cells about 45% at 50 μM[2]. E3330 (0-30 μM) inhibits the growth and migration of pancreatic cancer cells[3]. E3330 (0-30 μM) significantly enhances intracellular ROS level and inhibits CD44 expression in PANC1 cells[3].
Cell Proliferation Assay[1] Cell Line: | Human umbilical vein endothelial cells (HUVECs), murine pancreatic cancer associated endothelial cells (mPCECs), human endothelial progenitor cells (hEPCs) | Concentration: | 1, 5, and 10 μM (HUVECs); 1. 5, 10. 20. 30, 40, and 50 μM (mPCECs); 1, 5, 10, 15, 20, 25, and 30 μM (hEPCs) | Incubation Time: | 48 h | Result: | Inhibited the growth of HUVECs, PCECs and EPCs. |
Western Blot Analysis[1] Cell Line: | mPCECs | Concentration: | 1, 5, and 10 μM | Incubation Time: | 48 h | Result: | Inhibited the growth of HUVECs, PCECs and EPCs. |
Cell Viability Assay[2] Cell Line: | H1975 cells | Concentration: | 0, 5, 10, 20, 30, 40, and 50 μM | Incubation Time: | 72 h | Result: | Showed decreased cell viability in about 45% at 50 μM. |
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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[4]. E3330 (0-100 mg/kg, Orally, once) attenuates the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge[5].
Animal Model: | Sprague-Dawley rats (adult male, 150-175 g)[4] | Dosage: | 25 mg/kg | Administration: | Orally, 5 daily, five days each week for three weeks | Result: | Attenuated the cisplatin-induced decrease in capsaicin-induced vasodilatation in the rat hindpaw. |
Animal Model: | Male Fischer (F344/DuCrj) rats (160-190 g)[5] | Dosage: | 0, 10, 30, and 100 mg/kg | Administration: | Orally, 1 h, 6 h or 12 h after galactosamine challenge | Result: | Attenuated the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge. |
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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 120 mg/mL(317.07 mM;Need ultrasonic) 配制储备液 1 mM | 2.6423 mL | 13.2114 mL | 26.4229 mL | 5 mM | 0.5285 mL | 2.6423 mL | 5.2846 mL | 10 mM | 0.2642 mL | 1.3211 mL | 2.6423 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.50 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.50 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.50 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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