Ro 90-7501

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。

Ro 90-7501 

Ro 90-7501 是一种淀粉样 β42 (42) 原纤维组装抑制剂,可降低 42 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。

Ro 90-7501

Ro 90-7501 Chemical Structure

CAS No. : 293762-45-5

规格 价格 是否有货
10 mM * 1 mL in DMSO ¥880 询问价格 & 货期
5 mg ¥800 询问价格 & 货期
10 mg ¥1400 询问价格 & 货期
25 mg ¥3000 询问价格 & 货期
50 mg ¥5000 询问价格 & 货期
100 mg ¥8000 询问价格 & 货期

* Please select Quantity before adding items.

Ro 90-7501 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • Neuronal Signaling Compound Library
  • PI3K/Akt/mTOR Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Oxygen Sensing Compound Library
  • Glycolysis Compound Library
  • Cytoskeleton Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Phosphatase Inhibitor Library
  • Anti-Cancer Metabolism Compound Library
  • Neurodegenerative Disease-related Compound Library
  • Glucose Metabolism Compound Library

生物活性

Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces 42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response[2]. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner[3]. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells[4].

IC50 & Target[1][3]

Amyloid β42

 

ATM

 

Protein phosphatase 5

 

Apoptosis

 

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].

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.

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].

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: 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.

分子量

340.38

Formula

C20H16N6

CAS 号

293762-45-5

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 : 41.67 mg/mL (122.42 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9379 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°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 (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。

    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 (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 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]. Tamari K, et al. Ro 90-7501 Is a Novel Radiosensitizer for Cervical Cancer Cells that Inhibits ATM Phosphorylation. Anticancer Res. 2019 Sep;39(9):4805-4810.

    [2]. Guo F, et al. RO 90-7501 enhances TLR3 and RLR agonist induced antiviral response. PLoS One. 2012;7(10):e42583.

    [3]. Hong TJ, et al. Ro 90-7501 inhibits PP5 through a novel, TPR-dependent mechanism. Biochem Biophys Res Commun. 2017 Jan 8;482(2):215-220.

    [4]. Bohrmann B, et al. Self-assembly of beta-amyloid 42 is retarded by small molecular ligands at the stage of structural intermediates. J Struct Biol. 2000 Jun;130(2-3):232-46.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务