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- 详细信息
- 文献和实验
- 技术资料
- CAS号:
1338542-14-5
- 规格:
25mg/50mg/100mg
| 规格: | 25mg | 产品价格: | ¥8480.0 |
|---|---|---|---|
| 规格: | 50mg | 产品价格: | ¥11040.0 |
| 规格: | 100mg | 产品价格: | ¥14000.0 |
Product Introduction
Bioactivity
| 名称 | OTS964 |
| 描述 | OTS964 is a potent, orally active compound that operates as a highly selective inhibitor of TOPK with an IC 50 of 28 nM [1]. Additionally, it demonstrates significant inhibitory action against cyclin-dependent kinase CDK11, specifically binding to CDK11B with a K d of 40 nM [2]. |
| 体外活性 | OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation [1]. OTS964 (10 nM; 48 hours) increases cancer cell death [1]. OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner [3]. Cell Proliferation Assay [1] Cell Line: LU-99 cells Concentration: 10 nM Incubation Time: 48 hours Result: Suppressed cancer cell proliferation. Apoptosis Analysis [1] Cell Line: LU-99 cells Concentration: 10 nM Incubation Time: 48 hours Result: Increased cancer cell death. Western Blot Analysis [3] Cell Line: Hs683 cells, H4 cells Concentration: 0.1, 1, 2 μM Incubation Time: 24 and 48 hours Result: Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner. |
| 体内活性 | OTS964 (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression [1]. OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression [1]. Animal Model: Nude mice bearing LU-99 lung cancer cells [1] Dosage: 40 mg/kg Administration: Intravenously; on days 1, 4, 8, 11, 15, and 18 Result: The tumors continued shrinking even after the treatment and finally revealed complete regression. Animal Model: Nude mice bearing LU-99 lung cancer cells [1] Dosage: 50 or 100 mg/kg Administration: Oral administration; once every day for 2 weeks Result: Achieved complete tumor regression. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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