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

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

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.

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.

176.17

C₉H₈N₂O₂

90417-38-2

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

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

*

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

• [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.