Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SC144 是一种口服活性 gp130 抑制剂。它结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进一步抑制下游靶基因的表达。它对 gp130 配体触发的信号转导有明显的抑制作用,可诱导人卵巢癌细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 197 | 现货 | ||
5 mg | ¥ 452 | 现货 | ||
10 mg | ¥ 771 | 现货 | ||
25 mg | ¥ 1,460 | 现货 | ||
50 mg | ¥ 2,450 | 现货 | ||
100 mg | ¥ 3,970 | 现货 | ||
500 mg | ¥ 8,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 490 | 现货 |
产品描述 | SC144 is an orally active small-molecule gp130 inhibitor. |
靶点活性 | Gp130:< 1 μM (Cell assay) |
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] |
细胞实验 | MTT assay (Only for Reference) |
分子量 | 322.3 |
分子式 | C16H11FN6O |
CAS No. | 895158-95-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 27 mg/mL (83.8 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1027 mL | 15.5135 mL | 31.027 mL | 77.5675 mL |
5 mM | 0.6205 mL | 3.1027 mL | 6.2054 mL | 15.5135 mL | |
10 mM | 0.3103 mL | 1.5513 mL | 3.1027 mL | 7.7567 mL | |
20 mM | 0.1551 mL | 0.7757 mL | 1.5513 mL | 3.8784 mL | |
50 mM | 0.0621 mL | 0.3103 mL | 0.6205 mL | 1.5513 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SC144 895158-95-9 Apoptosis Immunology/Inflammation Interleukin SC-144 anti-angiogenesis Inhibitor oral inhibit SC 144 arrest translocation ovarian nuclear Interleukin Related phosphorylation cancer cell-cycle inhibitor