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SC144

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产品编号 T6207Cas号 895158-95-9

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。

SC144

SC144

Rating icon 很棒
纯度: 99.85%
产品编号 T6207Cas号 895158-95-9

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。

规格价格库存数量
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 x 10 mM (in DMSO)¥ 490现货
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产品介绍

生物活性
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)
化学信息
分子量322.3
分子式C16H11FN6O
CAS No.895158-95-9
SmilesCl.Fc1ccc2c(c1)nc(NNC(=O)c1cnccn1)c1cccn21
密度1.53 g/cm3 (Predicted)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 15 mg/mL (46.54 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
1mg5mg10mg50mg
1 mM3.1027 mL15.5135 mL31.0270 mL155.1350 mL
5 mM0.6205 mL3.1027 mL6.2054 mL31.0270 mL
10 mM0.3103 mL1.5513 mL3.1027 mL15.5135 mL
20 mM0.1551 mL0.7757 mL1.5513 mL7.7567 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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