E3330 APX-3330|cas:136164-66-4|西域试剂

E3330 APX-3330,99.34%

产品编号：Bellancom-19357| CAS NO：136164-66-4| 分子式：C₂₁H₃₀O₆| 分子量：378.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-19357	￥1190.00	杭州北京（现货）
Bellancom-19357	￥1950.00	杭州北京（现货）
Bellancom-19357	￥5500.00	杭州北京（现货）
Bellancom-19357	￥7990.00	杭州北京（现货）

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E3330 APX-3330

产品介绍

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^[4]^[5].

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 120 mg/mL (317.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。