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Rubitecan

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纯度: 97.54%

货号 T5853Cas号 91421-42-0

别名 鲁比特康, RFS 2000, 9-Nitrocamptothecin

Rubitecan (9-Nitrocamptothecin) 是一种与喜树碱相关的半合成药物,具有有效的抗肿瘤和抗病毒特性。它是一种 DNA 拓扑异构酶 I 抑制剂,以浓度依赖性方式抑制 DNA 拓扑异构酶 I 并在无细胞试验中增加超螺旋 DNA 的比例。

Rubitecan
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Rubitecan

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Rating icon 很棒

纯度: 97.54%

货号 T5853 别名 鲁比特康, RFS 2000, 9-NitrocamptothecinCas号 91421-42-0

Rubitecan (9-Nitrocamptothecin) 是一种与喜树碱相关的半合成药物,具有有效的抗肿瘤和抗病毒特性。它是一种 DNA 拓扑异构酶 I 抑制剂,以浓度依赖性方式抑制 DNA 拓扑异构酶 I 并在无细胞试验中增加超螺旋 DNA 的比例。

规格价格库存数量
1 mg
¥ 137
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5 mg
¥ 289
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10 mg
¥ 413
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25 mg
¥ 782
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50 mg
¥ 1,130
现货
100 mg
¥ 1,760
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200 mg
¥ 2,590
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1 mL x 10 mM (in DMSO)
¥ 318
现货
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产品介绍


Rubitecan AI Summary
Rubitecan is a lactone compound that exhibits a wide range of biological activities. It has demonstrated significant antitumor effects against P-338 leukemia in mice, extending the survival time of treated animals to 348% of control animals and achieving 5 cures within an active dose range of 2.5 to 20 mg/kg, with a toxic dose of 40 mg/kg. In lactone metabolism studies, Rubitecan causes a rapid decrease in lactone levels in human and mouse plasma, reaching 0% in humans and 18-30% in mice within a few hours. The compound shows potency in inhibiting ROR gamma transcriptional activity (89.1 nM to 631.0 nM), activities against the malarial parasite plastid, and inhibition of USP1/UAF1 (63095.7 nM). It induces apoptosis in human Caco2 cells with IC50 values between 112.0 nM and 479.0 nM and is active in assays involving Schwann cells and colon adenocarcinoma cells. Rubitecan also inhibits various human multidrug resistance-associated proteins (MRP2, MRP3, and MRP4) with varying IC50 values and has weak activity against human BSEP. While showing no significant antifungal or antibacterial effects, Rubitecan exhibits antiviral activity against SARS-CoV-2. It inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at a concentration of 10 µM, showing a reduction in cytotoxicity by 37.5% in Caco-2 cells but with relatively high IC50 values indicating weaker potency. Additionally, Rubitecan has limited binding affinity towards various human receptors and enzymes, with non-significant activity levels in most cases. It exhibits some antagonistic activity at human TBXA2R and weak inhibitory effects on human ACHE, but these are not prominent compared to its other bioactivities..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Rubitecan (9-Nitrocamptothecin) is a DNA topoisomerase I inhibitor. It inhibits DNA topoisomerase I and increases the fraction of supercoiled DNA in a cell-free assay in a concentration-dependent manner.Rubitecan is a semisynthetic agent related to camptothecin with potent antitumor and antiviral properties.
别名鲁比特康, RFS 2000, 9-Nitrocamptothecin
化学信息
分子量393.35
分子式C20H15N3O6
CAS No.91421-42-0
SmilesCC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cccc([N+]([O-])=O)c4cc3Cn1c2=O
密度1.63g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 50 mg/mL (127.11 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.17 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.5423 mL12.7113 mL25.4227 mL127.1133 mL
5 mM0.5085 mL2.5423 mL5.0845 mL25.4227 mL
10 mM0.2542 mL1.2711 mL2.5423 mL12.7113 mL
20 mM0.1271 mL0.6356 mL1.2711 mL6.3557 mL
50 mM0.0508 mL0.2542 mL0.5085 mL2.5423 mL
100 mM0.0254 mL0.1271 mL0.2542 mL1.2711 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20g,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%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/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 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | 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。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
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
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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