化合物SC144 T6207
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
500 mg | 895158-95-9 | ¥8,630.00 | 询底价 |
5 mg | 895158-95-9 | ¥452.00 | 询底价 |
50 mg | 895158-95-9 | ¥2,450.00 | 询底价 |
100 mg | 895158-95-9 | ¥3,970.00 | 询底价 |
25 mg | 895158-95-9 | ¥1,460.00 | 询底价 |
10 mg | 895158-95-9 | ¥771.00 | 询底价 |
1 mg | 895158-95-9 | ¥197.00 | 询底价 |
1 mL | 895158-95-9 | ¥490.00 | 询底价 |
Product Introduction
Bioactivity
英文名: SC144
描述: 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。
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
溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 27 mg/mL (83.8 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字: SC-144 | anti-angiogenesis | Apoptosis | Inhibitor | oral | inhibit | SC144 | SC 144 | arrest | translocation | ovarian | nuclear | Interleukin Related | phosphorylation | cancer | cell-cycle
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相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library | Target-Focused Phenotypic Screening Library | Nonsteroidal Anti-Inflammatory Compound Library | NO PAINS Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途