鸦胆子苦醇
基本信息
产品名称：
鸦胆子苦醇
英文名称：
Brusatol
国产/进口：
进口
产地/品牌：
美国/TargetMol
型号：
参考报价：
面议
销售商：
总点击数：
97
更新日期：
2025-05-27
产品类别：
性能参数
Product Introduction
Bioactivity
英文名: Brusatol
描述: Brusatol (NSC-172924) 是一种从鸦胆子植物中分离出来的天然产物，抑制Nrf2通路，可使多种癌细胞对 Cisplatin 和其他化疗药物敏感。它可开发为辅助化疗化合物，可增加细胞凋亡。
细胞实验: CT-26 cells in logarithmic growth are seeded onto a 96-well plate at a density of 4×10^3 cells/well. After 24 h of incubation at 37°C, fresh medium containing a series of concentrations of Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) and CDDP (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) is added at 100 μL/well; each concentration is used to treat six replicate wells. After 48 h of incubation at 37°C, the cells are further incubated with MTT (10 mg/mL) at 37°C for 4 h. The supernatant is then removed and the precipitate is dissolved with 100 μL DMSO. Absorbance is measured using a microplate reader at a wavelength of 490 nm. Cytotoxicity is expressed as the concentration of Brusatol and CDDP that inhibit cell growth by 50% (IC50 value). The inhibitory rate is calculated. The possible synergistic effect of Brusatol combined with CDDP is investigated by exposing CT-26 cells to various concentrations of each agent alone or in combination for 48 h [2].
动物实验: Athymic nude mice are used. Mice 4-6 wk old are injected with A549 cells. Once the tumors reached 80 mm3 (for the two times five-time Cisplatin treatment regimen) or 280 mm3 (for the single five-time Cisplatin treatment regime), mice are randomly allocated into four groups and treated i.p. with DMSO, Cisplatin (2 mg/kg), Brusatol (2 mg/kg), or in combination every other day for a total of five times. After the initial five-time Cisplatin treatment regimen, treatment stops for 1 wk to allow mice to recover before the second five-time Cisplatin treatment regimen is repeated [3].
体外活性: Brusatol 通过一种不依赖于 Keap1、蛋白酶体和自噬蛋白降解系统的机制，引发 Nrf2 的消耗。在小鼠 Hepa-1c1c7 肝癌细胞中，Brusatol 通过一种转录后机制迅速且短暂地引起 Nrf2 蛋白的消耗。Brusatol 也能抑制新鲜分离的原代人肝细胞中的 Nrf2 [1]。CT-26 细胞分别单独或联合应用不同浓度的 Brusatol（0.05、0.15、0.45、1.35、4.05 和 12.15 μg/mL）和 CDDP（0.05、0.15、0.45、1.35、4.05 和 12.15 μg/mL）处理 48 小时。经 Brusatol 和 CDDP 处理 48 小时后，CT-26 细胞的存活率呈剂量依赖性降低，其 IC50 值分别为 0.27±0.01 和 1.44±0.22 μg/mL。当 Brusatol 与 CDDP 以 1:1 的恒定浓度比联合应用时，细胞生长抑制明显增强，合用治疗的 IC50 值为 0.19±0.02 μg/mL [2]。
体内活性: 裸鼠被注射A549细胞以诱导肿瘤生长，随后进行一次每千克体重2 mg的Brusatol腹腔注射。在注射后24小时或48小时，将肿瘤组织分离出来。发现Nrf2蛋白水平在注射后24小时或48小时显著降低，表明Brusatol能够达到肿瘤组织并抑制Nrf2途径。在第一次实验中，一旦肿瘤体积达到平均230 mm3，将DMSO、Brusatol（每千克体重2 mg）、Cisplatin（每千克体重2 mg）或Cisplatin（每千克体重2 mg）与Brusatol（每千克体重2 mg）联合治疗通过腹腔注射，每隔一天一次，共五次。Cisplatin或Brusatol单独使用未能显著抑制肿瘤生长，而在联合治疗组中，肿瘤体积显著减小[3]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : Insoluble
DMSO : 90 mg/mL (172.9 mM)
关键字: Nrf2 | oxygen | CT-26 | defense | stress | Keap1-Nrf2 | Brusatol | chemosensitization | Toxicity | NSC-172924 | species | radicals | reactive | Chemical | response | cisplatin | synergistic effect | Hepatocyte | Keap1 | antioxidant | Cell | Free | Inhibitor | inhibit | NSC172924 | Apoptosis
相关产品: Bay 11-7085 | DL-Buthionine-(S,R)-sulfoximine | Deferasirox | Alogliptin | FA16 | Acetylcysteine | DL-Glutamine | (-)-Epicatechin | Pifithrin-α hydrobromide | BAY 87-2243
相关库: Anti-Tumor Natural Product Library | Terpene Natural Product Library | Covalent Natural Product Library | Ferroptosis Compound Library | Human Metabolite Library | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | Antiparasitic Natural Product Library | Covalent Inhibitor Library
Bioactivity
英文名: Brusatol
描述: Brusatol (NSC-172924) 是一种从鸦胆子植物中分离出来的天然产物，抑制Nrf2通路，可使多种癌细胞对 Cisplatin 和其他化疗药物敏感。它可开发为辅助化疗化合物，可增加细胞凋亡。
细胞实验: CT-26 cells in logarithmic growth are seeded onto a 96-well plate at a density of 4×10^3 cells/well. After 24 h of incubation at 37°C, fresh medium containing a series of concentrations of Brusatol (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) and CDDP (0.05, 0.15, 0.45, 1.35, 4.05 and 12.15 μg/mL) is added at 100 μL/well; each concentration is used to treat six replicate wells. After 48 h of incubation at 37°C, the cells are further incubated with MTT (10 mg/mL) at 37°C for 4 h. The supernatant is then removed and the precipitate is dissolved with 100 μL DMSO. Absorbance is measured using a microplate reader at a wavelength of 490 nm. Cytotoxicity is expressed as the concentration of Brusatol and CDDP that inhibit cell growth by 50% (IC50 value). The inhibitory rate is calculated. The possible synergistic effect of Brusatol combined with CDDP is investigated by exposing CT-26 cells to various concentrations of each agent alone or in combination for 48 h [2].
动物实验: Athymic nude mice are used. Mice 4-6 wk old are injected with A549 cells. Once the tumors reached 80 mm3 (for the two times five-time Cisplatin treatment regimen) or 280 mm3 (for the single five-time Cisplatin treatment regime), mice are randomly allocated into four groups and treated i.p. with DMSO, Cisplatin (2 mg/kg), Brusatol (2 mg/kg), or in combination every other day for a total of five times. After the initial five-time Cisplatin treatment regimen, treatment stops for 1 wk to allow mice to recover before the second five-time Cisplatin treatment regimen is repeated [3].
体外活性: Brusatol 通过一种不依赖于 Keap1、蛋白酶体和自噬蛋白降解系统的机制，引发 Nrf2 的消耗。在小鼠 Hepa-1c1c7 肝癌细胞中，Brusatol 通过一种转录后机制迅速且短暂地引起 Nrf2 蛋白的消耗。Brusatol 也能抑制新鲜分离的原代人肝细胞中的 Nrf2 [1]。CT-26 细胞分别单独或联合应用不同浓度的 Brusatol（0.05、0.15、0.45、1.35、4.05 和 12.15 μg/mL）和 CDDP（0.05、0.15、0.45、1.35、4.05 和 12.15 μg/mL）处理 48 小时。经 Brusatol 和 CDDP 处理 48 小时后，CT-26 细胞的存活率呈剂量依赖性降低，其 IC50 值分别为 0.27±0.01 和 1.44±0.22 μg/mL。当 Brusatol 与 CDDP 以 1:1 的恒定浓度比联合应用时，细胞生长抑制明显增强，合用治疗的 IC50 值为 0.19±0.02 μg/mL [2]。
体内活性: 裸鼠被注射A549细胞以诱导肿瘤生长，随后进行一次每千克体重2 mg的Brusatol腹腔注射。在注射后24小时或48小时，将肿瘤组织分离出来。发现Nrf2蛋白水平在注射后24小时或48小时显著降低，表明Brusatol能够达到肿瘤组织并抑制Nrf2途径。在第一次实验中，一旦肿瘤体积达到平均230 mm3，将DMSO、Brusatol（每千克体重2 mg）、Cisplatin（每千克体重2 mg）或Cisplatin（每千克体重2 mg）与Brusatol（每千克体重2 mg）联合治疗通过腹腔注射，每隔一天一次，共五次。Cisplatin或Brusatol单独使用未能显著抑制肿瘤生长，而在联合治疗组中，肿瘤体积显著减小[3]。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : Insoluble
DMSO : 90 mg/mL (172.9 mM)
关键字: Nrf2 | oxygen | CT-26 | defense | stress | Keap1-Nrf2 | Brusatol | chemosensitization | Toxicity | NSC-172924 | species | radicals | reactive | Chemical | response | cisplatin | synergistic effect | Hepatocyte | Keap1 | antioxidant | Cell | Free | Inhibitor | inhibit | NSC172924 | Apoptosis
相关产品: Bay 11-7085 | DL-Buthionine-(S,R)-sulfoximine | Deferasirox | Alogliptin | FA16 | Acetylcysteine | DL-Glutamine | (-)-Epicatechin | Pifithrin-α hydrobromide | BAY 87-2243
相关库: Anti-Tumor Natural Product Library | Terpene Natural Product Library | Covalent Natural Product Library | Ferroptosis Compound Library | Human Metabolite Library | Inhibitor Library | Traditional Chinese Medicine Monomer Library | Anti-Cancer Active Compound Library | Antiparasitic Natural Product Library | Covalent Inhibitor Library
公司简介
TargetMol（陶术）作为一家全球性的生物医药领域高科技企业，我们致力于为高校、研究所、医院、企业等各类生物医药研发机构提供优质的产品和服务，为全球医药科学家更高效地完成科研工作助力。可提供20,000+种 抑制剂和激动剂 、800+种 化合物库 、19,000+种 天然产物 ，以及9,000+种 重组蛋白 、多种 多肽 、抗体 和 生命科学试剂盒 等。此外，在上海，TargetMol研发中心配备了 CADD & AIDD研究中心、药理实验室和药物化学合成 平台三大技术中心，可提供虚拟筛选、化合物活性测试、分子间结合力检测和化合物结构优化等技术服务，多方位满足用户的研发需求。
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