Ro 90-7501 是一种淀粉样 β42(Aβ42) 原纤维组装抑制剂,可降低Aβ42诱导的细胞毒性 (EC50为 2 μM)。Ro 90-7501 抑制ATM磷酸化和 DNA 修复。RO 90-7501选择性增强 TLR3 和 RLR 配体诱导的 IFN-β 基因表达和抗病毒反应。Ro 90-7501 还以 TPR 依赖性方式抑制蛋白磷酸酶 5 (PP5),并对宫颈癌细胞具有显着的放射增敏作用。
生物活性 | Ro 90-7501 is anamyloid β42(Aβ42) fibril assemblyinhibitor that reducesAβ42-induced cytotoxicity (EC50of 2 μM). Ro 90-7501 inhibitsATMphosphorylation and DNA repair. RO 90-7501 selectively enhancestoll-like receptor 3(TLR3) andRIG-I-like receptor(RLR) ligand-induced IFN-β gene expression and antiviral response[2]. Ro 90-7501 also inhibitsproteinphosphatase5 (PP5)in a TPR-dependent manner[3]. Ro 90-7501 has significant radiosensitizing effects on cervicalcancercells[4]. |
IC50& Target[1][3] | Amyloid β42 | ATM | Protein phosphatase 5 | Apoptosis |
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体外研究 (In Vitro) | Ro 90-7501 significantly enhances radiosensitivity compared with control HeLa and ME-180 cells. Ro 90-7501 significantly increases apoptosis and impaired cell cycle after irradiation. Ro 90-7501 suppresses the phosphorylation of ATM and its downstream proteins, such as H2AX, Chk1, and Chk2, after irradiation[1]. RO 90-7501, itself affects neither IFN-β nor NFκB promoter activity, but significantly enhances poly I:C-induced IFN-β promoter activation and inhibits the activation of NFκB in a dose-dependent manner. Treatment of cells with RO 90-7501 significantly enhances the antiviral activity of poly I:C[2].
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体内研究 (In Vivo) | Ro 90-7501 (5 μg/g; intraperitoneal injection; daily; for 21 days; female BALB/c nude mice) treatment significantly delays tumor growth and significantly decreases tumor volume[1].
Animal Model: | Female BALB/c nude mice (8-week-old) with HeLa cells under irradiation[1] | Dosage: | 5 μg/g | Administration: | Intraperitoneal injection; daily; for 21 days | Result: | Tumor growth was significantly delayed in the combination group. Tumor volume was also significantly decreased in the irradiation group. |
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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 |
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溶解性数据 | In Vitro: DMSO : 41.67 mg/mL(122.42 mM;Need ultrasonic) 配制储备液 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL | 5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL | 10 mM | 0.2938 mL | 1.4689 mL | 2.9379 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。-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 (6.11 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (6.11 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 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 (6.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.11 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。 *以上所有助溶剂都可在本网站选购。
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