NU1025

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

NU1025  纯度: ≥98.0%

NU1025 是一种有效的 PARP 抑制剂,IC50 为 400 nM,Ki 为 48 nM。NU1025 可增强电离辐射和抗癌药物的细胞毒性,并具有抗癌和神经保护的作用。

NU1025

NU1025 Chemical Structure

CAS No. : 90417-38-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1320 In-stock
10 mg ¥1200 In-stock
50 mg ¥4000 In-stock
100 mg ¥6500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NU1025 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Epigenetics Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Neuroprotective Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library

生物活性

NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity[1][2][3].

IC50 & Target

IC50: 400 nM (PARP)[2]
Ki: 48 nM (PARP)[3]

体外研究
(In Vitro)

NU1025 (0.2 mM) pretreatment restores cell viability to approximately 73% and 82% in H2O2 and SIN-1 injured cells, respectively[1].
NU1025 enhances the cytotoxicity of the DNA-methylating agent MTIC, γ-irradiation and bleomycin 3.5-, 1.4- and 2-fold respectively in L1210 cells. The recovery from potentially lethal γ-irradiation damage cytotoxicity in plateau-phase cells is also inhibited by NU 1025. NU1025 causes a marked retardation of DNA repair[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 0.2 mM
Incubation Time: 6.5 hours
Result: Restored cell viability to approximately 73% and 82% in H2O2 and SIN-1 injured cells.

体内研究
(In Vivo)

NU1025 (1-3 mg/kg; intraperitoneal injection; male Sprague Dawley rats) treatment at 1 and 3 mg/kg reduces total infarct volume to 25% and 45%, respectively, when administered 1 h before reperfusion. NU1025 also produces significant improvement in neurological deficits. Neuroprotection with NU1025 is associated with reduction in PAR accumulation, reversal of brain NAD depletion and reduction in DNA fragmentation[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley rats (250-270 g) induced focal cerebral ischemia[1]
Dosage: 1 mg/kg, 3 mg/kg
Administration: Intraperitoneal injection
Result: At 1 and 3 mg/kg, reduced total infarct volume to 25% and 45%, respectively.

分子量

176.17

Formula

C9H8N2O2

CAS 号

90417-38-2

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
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (709.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.6763 mL 28.3817 mL 56.7634 mL
5 mM 1.1353 mL 5.6763 mL 11.3527 mL
10 mM 0.5676 mL 2.8382 mL 5.6763 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 (11.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.81 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 (11.81 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (11.81 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Kaundal RK, et al. Neuroprotective effects of NU1025, a PARP inhibitor in cerebral ischemia are mediated through reduction in NAD depletion and DNA fragmentation. Life Sci. 2006 Nov 10;79(24):2293-302.

    [2]. Bowman KJ, et al. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064. Br J Cancer. 1998 Nov;78(10):1269-77.

    [3]. Delaney CA, et al. Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines. Clin Cancer Res. 2000 Jul;6(7):2860-7.

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