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- CAS号:
895158-95-9
- 规格:
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/500mg
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥392.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥173.0 |
| 规格: | 5mg | 产品价格: | ¥361.0 |
| 规格: | 10mg | 产品价格: | ¥616.0 |
| 规格: | 25mg | 产品价格: | ¥1168.0 |
| 规格: | 50mg | 产品价格: | ¥1960.0 |
| 规格: | 100mg | 产品价格: | ¥3176.0 |
| 规格: | 500mg | 产品价格: | ¥6904.0 |
Product Introduction
Bioactivity
| 名称 | SC144 |
| 描述 | SC144 is an orally active small-molecule gp130 inhibitor. |
| 细胞实验 | MTT assay (Only for Reference) |
| 体外活性 | SC144 exhibits potent cytotoxicity against a panel of drug-sensitive and drug-resistant cancer cell lines. SC144 shows synergism with both 5-fluorouracil and oxaliplatin when co-treated in colorectal cancer HT29 cells. Pretreatment with SC144 in oxaliplatin-resistant HTOXAR3 cells is more effective than oxaliplatin pretreatment. In addition, the combination of SC144 and paclitaxel exhibited synergism in MDA-MB-435 cells with a schedule-dependent block in cell cycle. [1] SC144 treatment in vitro induces gp130 phosphorylation and deglycosylation, resulting in the downregulation of surface-bound gp130 and the abrogation of gp130-associated Stat3 activation. In addition, SC144 selectively inhibits the downstream signaling activation induced by gp130 substrates, including IL-6 and LIF. Protein expression regulated by the gp130/Stat3 axis in OVCAR-8 cells is also down-regulated after SC144 treatment, including Bcl-2, Bcl-XL, survivin, cyclin D1, MMP-7, gp130 and Ape1/Rel-1. [2] |
| 体内活性 | SC144 significantly inhibits tumor growth in a mouse xenograft model of human ovarian cancer via i.p. or p.o. administration. After SC144 treatment for two months, gp130, Bcl-2, Bcl-XL, MMP-7 and Ape1/Ref-1 protein levels are substantially decreased in the tumor site in the treatment group compared with the control group. [2] In an MDA-MB-435 mouse xenograft model, co-administration of SC144 and paclitaxel delays tumor growth in an SC144 dose-dependent manner. Evaluation of the pharmacokinetics of SC144 reveals that intraperitoneal administration of SC144 shows a two-compartmental pharmacokinetics elimination profile that is not observed in the oral dosing. [1] |
| 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. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 15 mg/mL (46.54 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
| 关键字 | translocation | SC-144 | SC144 | SC 144 | phosphorylation | ovarian | oral | nuclear | Interleukin Related | Interleukin | Inhibitor | inhibit | gp130 | cell-cycle | cancer | arrest | Apoptosis | anti-angiogenesis |
| 相关产品 | Formamide | Urea | Kaolin | Aceglutamide | Alginic acid | Metronidazole | Sildenafil citrate | Stavudine | Gluconate Calcium | Tamoxifen | D(+)-Raffinose pentahydrate | Hydroxypropyl Cellulose |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Apoptosis Compound Library | Anti-Ovarian Cancer Compound Library | Nonsteroidal Anti-Inflammatory Compound Library | NO PAINS Compound Library | Hematonosis Compound Library | Immunology/Inflammation Compound Library | Target-Focused Phenotypic Screening Library |
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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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