• 产品描述： 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

• 靶点： Ape-1, Ref-1;HIF/HIFProlyl-Hydroxylase; DNA/RNASynthesis

• 体外研究：
  E3330 (0-50 μM，48 h) 抑制 HUVECs、PCECs 和 EPCs 的生长。 E3330 (0-5 μM) 减少分泌的和细胞内的 VEGF (血管内皮生长因子) 表达，同时下调 PCECs 上的同源受体 Flk-1/KDR。 E3330 (0-1 μM) 抑制骨髓间充质细胞分化干细胞 (BM-MSCs) 进入内皮谱系的 CD31+ 细胞。 E3330 (0-50 μM，72 小时) 降低细胞活力H1975 细胞约 45% 在 50 μM。 E3330 (0-30 μM) 抑制胰腺癌细胞的生长和迁移。 E3330 (0-30 μM) 显著提高细胞内 ROS 水平并抑制 PANC1 细胞中的 CD44 表达 Cell Proliferation Assay 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 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 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.

• 体内研究：
  E3330 (25 mg/kg，口服，每天 5 次，每周 5 天，持续三周) 对顺铂引起的辣椒素诱导的血管舒张改变具有神经保护作用。 E3330 (0-100 mg/kg，口服，一次) 在半乳糖胺攻击后 1 小时、6 小时或 12 小时给予可减轻肝损伤。 Animal Model: Sprague-Dawley rats (adult male, 150-175 g) 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.

• 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. 3. Zou GM, et al. Small-molecule inhibitor of the AP endonuclease 1/REF-1 E3330 inhibits pancreatic cancer cell growth and migration. Mol Cancer Ther. 2008 Jul;7(7):2012-21. 4. Kelley MR, et al. Role of the DNA base excision repair protein, APE1 in cisplatin, oxaliplatin, or carboplatin induced sensory neuropathy. PLoS One. 2014 Sep 4;9(9):e106485. 5. Nagakawa J, et al. Protective effect of E3330, a novel quinone derivative, in galactosamine-induced hepatitis in rats. J Pharmacol Exp Ther. 1993 Jan;264(1):496-500.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.642 ml	13.211 ml	26.423 ml
  5 mM	0.528 ml	2.642 ml	5.285 ml
  10 mM	0.264 ml	1.321 ml	2.642 ml
  50 mM	0.053 ml	0.264 ml	0.528 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *