PARP1-IN-5 dihydrochloride 是一种低毒、具有口服活性、有效的和有选择性的PARP-1抑制剂(IC50=14.7 nM)。PARP1-IN-5 dihydrochloride 可用于癌症研究。
生物活性 | PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selectivePARP-1inhibitor (IC50=14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research ofcancer[1]. |
IC50& Target[1] | PARP-1 14.7 nM (IC50) | PARP-2 0.9 μM (IC50) |
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体外研究 (In Vitro) | PARP1-IN-5 dihydrochloride (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 dihydrochloride (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 dihydrochloride (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 dihydrochloride (SK-OV-3 cells) can significantly decrease the PAR level[1]. PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression[1].
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体内研究 (In Vivo) | PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1]. PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg[1]. PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1]. PARP1-IN-5 dihydrochloride can upregulate the expression of γ-H2AX and decrease the expression of PAR[1].
Animal Model: | Mice[1] | Dosage: | 1000 mg/kg | Administration: | P.o. | Result: | There was no significant difference in the body weight and blood routine. |
Animal Model: | Mice[1] | Dosage: | 25 and 50 mg/kg | Administration: | P.o.; 12 days | Result: | Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg. |
Animal Model: | Male Sprague–Dawley (SD) rats[1] | Dosage: | 50 mg/kg (Pharmacokinetic Analysis) | Administration: | P.o. | Result: | Positively correlated with the expression of PARP-1. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 125 mg/mL(232.58 mM;Need ultrasonic) H2O : 1 mg/mL(1.86 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 1.8606 mL | 9.3030 mL | 18.6060 mL | 5 mM | 0.3721 mL | 1.8606 mL | 3.7212 mL | 10 mM | 0.1861 mL | 0.9303 mL | 1.8606 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 (sealed storage, away from moisture)。-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 (3.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.87 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 (3.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.87 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 (3.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.87 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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