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Rafoxanide

Rafoxanide

产品编号 T7093   CAS 22662-39-1
别名: 碘醚柳胺, 雷复尼特

Rafoxanide 是口服活性水杨酰苯胺类驱虫剂。它作为抗寄生虫剂,可用于控制羊和牛的 Hemonchus 种和 Fasciola 种的感染。

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Rafoxanide Chemical Structure
Rafoxanide, CAS 22662-39-1
规格 价格/CNY 货期 数量
100 mg ¥ 194 现货
500 mg ¥ 418 现货
1 g ¥ 713 现货
1 mL * 10 mM (in DMSO) ¥ 460 现货
其他形式的 Rafoxanide:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Rafoxanide (T7093)
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参考文献
产品描述 Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.
体外活性 Rafoxanide exhibit a high cytotoxic effects (IC50: 1.09 μM for A375 and 1.31 μM for A431 cells).?Consistent with the expected properties of CDK4/6 inhibitors, rafoxanide significantly increased the G1 phase population.?Notably, Rafoxanide specifically decreased the expression of CDK4/6, cyclin D, retinoblastoma protein (Rb) and the phosphorylation of CDK4/6 and Rb[1].
体内活性 Rafoxanide specifically decreased the expression of CDK4/6, cyclin D, retinoblastoma protein (Rb) and the phosphorylation of CDK4/6 and Rb. Furthermore, the anticancer effect of rafoxanide was demonstrated in vivo in BALB/C nude mice subcutaneously xenografted with human skin cancer A375 cells. Rafoxanide (40 mg/kg, i.p.) exhibited significant antitumor activity, comparable to that of oxaliplatin (5 mg/kg, i.p.). The combined administration of rafoxanide and oxaliplatin produced a synergistic therapeutic effect. First to indicate that rafoxanide inhibits CDK4/6 activity and is a potential candidate drug for the treatment of human skin cancer[1].
细胞实验 Cell cycle analysis using an EPICS XL4 Flow Cytometer.?The cell cycle phase distribution was analyzed using ModFit LT 2.0 software.?Briefly, cells (4x10^4 ) were seeded in 24-well plates in DMEM containing 0.125% FBS.?After 24 h, the cell culture medium was replaced with DMEM containing 10% FBS and various doses of rafoxanide (1, 3, 10 or 30 μM) for 6, 12 or 24 h, as indicated.?At the end of the experiments, cells (1x10^4 ) were fixed in ice cold 70% ethanol, and stained using a Coulter DNA Prep Reagent kit , and cellular DNA content was assessed.?All data were obtained from two separate experiments performed in triplicate[1]
动物实验 A375 cells (1x10^6 ) were suspended in 0.2 ml PBS, and injected subcutaneously into the right flank of the mice (n=3).?Tumor size was assessed using a caliper.?When the tumors grew to 80-100 mm^3 (1 week after inoculation), mice were divided randomly into different experimental groups (5 mice/group), and intraperitoneally injected daily for 21 days with various testing compounds(Rafoxanide).?The mice were sacrificed by cervical dislocation, and the tumors were excised, weighed, and images were captured by camera .?The tumor volume was calculated using the formula V = ab^2 /2 (a = longest axis;?b = shortest axis)[1].
别名 碘醚柳胺, 雷复尼特
分子量 626.01
分子式 C19H11Cl2I2NO3
CAS No. 22662-39-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 31 mg/mL (49.52 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5974 mL 7.9871 mL 15.9742 mL 39.9355 mL
5 mM 0.3195 mL 1.5974 mL 3.1948 mL 7.9871 mL
10 mM 0.1597 mL 0.7987 mL 1.5974 mL 3.9935 mL
20 mM 0.0799 mL 0.3994 mL 0.7987 mL 1.9968 mL

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TargetMol Library Books参考文献

1. Shi X, Li H, Shi A et al.Discovery of rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer[J].Oncol Rep. 2018 Sep;40(3):1592-1600. 2. Xiao W , Xu Z , Chang S , et al. Rafoxanide, an organohalogen drug, triggers apoptosis and cell cycle arrest in multiple myeloma by enhancing DNA damage responses and suppressing the p38 MAPK pathway[J]. Cancer Letters, 2019, 444:45-59.
Palbociclib monohydrochloride CDK9 inhibitor HH1 Lerociclib VX-11e AG-024322 A-443654 THZ1 Avotaciclib

相关化合物库

该产品包含在如下化合物库中:
抗寄生虫库 抑制剂库 激酶抑制剂库 抗前列腺癌化合物库 FDA上市及药典收录分子库 细胞周期化合物库 抗乳腺癌化合物库 抗胰腺癌化合物库 已知活性化合物库 经典已知活性库

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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。

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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。

Keywords

Rafoxanide 22662-39-1 Cell Cycle/Checkpoint Microbiology/Virology CDK Parasite 碘醚柳胺 Hemonchus energy metabolism inhibit antiparasitic Fasciola Estrus ovis halogenated salicylaniline 雷复尼特 uncoupling oxidative phosphorylation Inhibitor inhibitor

 

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