Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Camptothecin (CPT) 属于生物碱类天然产物,是一种 DNA 拓扑异构酶 I (Topo I) 的抑制剂 (IC50=679 nM),具有特异性。Camptothecin 具有抗肿瘤活性,可以诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
20 mg | ¥ 140 | 现货 | ||
50 mg | ¥ 220 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 160 | 现货 |
产品描述 | Camptothecin (CPT) belongs to the alkaloid group of natural products and is a specific DNA topoisomerase I (Topo I) inhibitor (IC50=679 nM) with specificity. Camptothecin has antitumor activity and induces apoptosis. |
靶点活性 | Topo I:0.68 μM |
体外活性 |
方法:八株 TNBC 细胞系用 Camptothecin (0.1-5 µM) 处理 72 h,使用 PrestoBlue 检测细胞活力。 结果:Camptothecin 抑制 MCF7、HCC1428、HCC1419、HCC202、MDA453、MDA231、Sum149、BT549 细胞活力,IC50 值分别为 0.089/0.448/0.067/0.481/0.058/0.040/0.065/0.056 µM。[1] 方法:肺癌细胞 H1299 和 H460 用 Camptothecin (0.5-5 µM) 处理 16 h,使用 wound-healing assay 检测细胞迁移情况。 结果:Camptothecin 抑制 H1299 和 H460 细胞迁移,但没有剂量依赖性作用。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Camptothecin (0.15-1.2 mg/kg) 和 doxorubicin (0.25-2 mg/kg) 静脉注射给携带三阴性乳腺癌肿瘤 MDA-MB-231 的 athymic nu/n 小鼠,每两天一次,给药四次。 结果:观察到肿瘤生长的剂量依赖性减少,在 0.5 mg/kg DOX + 0.3 mg/kg CPT 下减少 40.8% ,在 1.5 mg/kg DOX + 0.9 mg/kg CPT 下减少 93%。最高的测试剂量 (2 mg/kg DOX + 1.2 mg/kg CPT) 在第 44 天完全停止了肿瘤的生长。[3] 方法:为研究对肥胖的作用,将 Camptothecin (1 mg/kg,0.1% Tween 80) 口服给药给肥胖小鼠,每天一次,持续三天。 结果:口服 Camptothecin 可增加饮食诱导肥胖 (DIO) 小鼠和遗传 ob/ob 小鼠的循环 GDF15 水平。与 GDF15 的厌食作用一致,Camptothecin 抑制食物摄入,从而降低肥胖小鼠的体重、血糖和肝脏脂肪含量。[4] |
激酶实验 | Topoisomerase I Cleavable Complex Assay: Topoisomerase I is isolated from calf thymus and is devoid of topoisomerase II. All reactions are carried out in 10 mL volumes of reaction buffer (50 mM Tris-HCl, pH 7.5, 100 mM KCl, 0.5 mM EDTA, and 30 pg/mL BSA) in microtiter plates. Camptothecin is dissolved in DMSO at 10 mg/mL and serially diluted in 96-well microtiter plates to which the 32P end-labeled pBR322 DNA and topoisomerase enzyme are added. The reaction mixture is incubated at room temperature for 30 min and then the reaction stopped by adding 2 mL of a mixture of sodium dodecyl sulfate and proteinase K (1.6% and 0.14 mg/mL final concentrations, respectively). The plates are heated at 50 °C for 30 min, 10 mL of standard stop mixture containing 0.45 N NaOH is added in order to generate single-stranded DNA, and the samples are electrophoresed in 1.5% agarose gels in TBE buffer. Gels are blotted on nitrocellulose paper, dried, and exposed to X-ray film. The units of cleavage are calculated from the autoradiographs and plotted against the log drug concentration. The IC50 values are then obtaine |
细胞实验 | Tumor cells are plated in 100 μL of medium in 96-well microtiter plates at a density of 1500 to 4000 cells per well and allowed to adhere overnight. Cells are incubated with Camptothecin for 48 hours and then with fresh medium for 48 hours. Camptothecin at each concentration is added in quadruplicate. Following a 4-hour incubation of treated cells with MTT, the reduced dye product is extracted from the cells with 0.2 mL of DMSO followed by 50 μL of Sorensen's buffer. The plates are shaken briefly, and the absorbance at 570 nm is read and quantitated. Curves are fitted to the MTT assay data using a four-parameter logistic equation.(Only for Reference) |
别名 | NSC-100880, Campathecin, 喜树碱, (S)-(+)-Camptothecin, CPT |
分子量 | 348.35 |
分子式 | C20H16N2O4 |
CAS No. | 7689-03-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.48 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8707 mL | 14.3534 mL | 28.7068 mL | 71.7669 mL |
5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL | 14.3534 mL | |
10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL | 7.1767 mL |
中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
胡麻叶 | Sesamum indicum DC. | 寒 | 甘 | |
硫球蛇根草 | Ophiorrhiza japonica Bl. | 平 | 淡 | 肝 |
毛泡桐 | Paulownia tomentosa (Thunb.) Steud. | - | ― | |
平车前 | Plantago depressa Willd. | 寒 | 甘 | |
蛇根草 | Ophiorrhiza japonica Blume | 平 | 淡 | 肝 |
喜树 | Camptotheca acuminata Decne. | 凉 | 苦, 涩 | 脾, 胃, 肝 |
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。
Camptothecin 7689-03-4 Apoptosis DNA Damage/DNA Repair Microbiology/Virology Antibiotic Topoisomerase Influenza Virus Antifungal NSC100880 HIF-1α Inhibitor ADC Payload DNA topoisomerase I microRNAs NSC 100880 NSC-100880 Top1 miRNA Campathecin inhibit 喜树碱 (S)-(+)-Camptothecin alkaloid miRN MicroRNA Fungal ADC Cytotoxin CPT inhibitor