Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cucurbitacin I (JSI-124) 是从曲莲中提取的一种天然产物,是 JAK2/STAT3选择性抑制剂,有抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 760 | 现货 | ||
5 mg | ¥ 3,610 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 4,120 | 现货 |
产品描述 | Cucurbitacin I (JSI-124), a natural compound, is a selective inhibitor of JAK2/STAT3 with anti-cancer activity. |
体外活性 | The anticancer activity of Cucurbitacin I is accomplished by downregulating p-STAT3 and MMP-9 expression [1]. Incubation of the Seax cell line with the Jak/Stat3 inhibitor Cucurbitacin I result in a time- and concentration-dependent decrease of P-Stat3 and Stat3. Incubation of freshly isolated Sz cells with 30 μM Cucurbitacin I for 6 hours induces apoptosis in the large majority (73-91%) of tumor cells [2]. PE-induced cell enlargement and upregulation of ANF and β-MHC are significantly suppressed by pretreatment of the cardiomyocytes with Cucurbitacin I. Cucurbitacin I also impaired connective tissue growth factor (CTGF) and MAPK signaling, pro-hypertrophic factors, as well as TGF-β/Smad signaling, the important contributing factors to fibrosis [3]. |
体内活性 | The differences in tumor volume between the Cucurbitacin I and control, combination and control, and combination and Cucurbitacin I arms are significant. Furthermore, combination-treated tumors exhibit a significantly lower average tumor weight at study termination than control. Moreover, there was no effect on the body weights of mice [4]. |
动物实验 | BALB/c nude (nu/nu) female mice are used. U251 cells (5×10^6 cells in 50 μL of serum-free DMEM) are inoculated subcutaneously into the right flank of 5-week-old female mice after acclimatization for a week. Tumor growth is measured daily with calipers. When the tumors reach a mean volume of 90-120 mm3, animals are randomized into groups. In the first experiment, 16 mice are randomly assigned to Cucurbitacin I (1 mg/kg/day in 20% DMSO in PBS) or drug vehicle control (20% DMSO in PBS) and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 18 days, whereas, in the second, 20 mice are assigned to four groups. Control animals receive 20% DMSO in PBS vehicle, whereas treated animals are injected with Cucurbitacin I (1 mg/kg/day) in 20% DMSO in PBS, CQ (25 mg/kg/day) in 20% DMSO in PBS, and Cucurbitacin I (1 mg/kg/day) plus CQ (25 mg/kg/day) in 20% DMSO in PBS and dosed intraperitoneally with 100 μL of vehicle or drug once daily for 15 days [4]. |
别名 | NSC-521777, JSI-124, Elatericin B, 葫芦素 I |
分子量 | 514.65 |
分子式 | C30H42O7 |
CAS No. | 2222-07-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (184.59 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9431 mL | 9.7153 mL | 19.4307 mL | 48.5767 mL |
5 mM | 0.3886 mL | 1.9431 mL | 3.8861 mL | 9.7153 mL | |
10 mM | 0.1943 mL | 0.9715 mL | 1.9431 mL | 4.8577 mL | |
20 mM | 0.0972 mL | 0.4858 mL | 0.9715 mL | 2.4288 mL | |
50 mM | 0.0389 mL | 0.1943 mL | 0.3886 mL | 0.9715 mL | |
100 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4858 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。
Cucurbitacin I 2222-07-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK STAT NSC-521777 Janus kinase NSC521777 Inhibitor JSI-124 Elatericin B JSI124 JSI 124 葫芦素 I NSC 521777 inhibit inhibitor