Camptothecin
作者：齊岳
發(fā)布時間：2023-09-05
08:53:56
點擊數(shù)：
產(chǎn)品名稱：Camptothecin
產(chǎn)品描述：
| 植物來源 | 天然產(chǎn)物 > 藍果樹科 > 喜樹屬 |
| 結構類型 | 天然產(chǎn)物 > 生物堿 |
| 產(chǎn)品描述 | (S)-(+)-Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I), isolated from Camptotheca acuminata. |
| 靶點活性 | Topo I:0.68 μM |
| 體外活性 | 在攜帶結腸癌,肺癌,乳腺癌,胃癌,和卵巢癌等移植瘤的小鼠中,Camptothecin（8 mg/kg ）能夠抑制腫瘤細胞生長. |
| 體內活性 | 在HCT116細胞中,Camptothecin（5 μM）誘導蛋白酶體介導的MLL5蛋白降解,其導致Ser392處p53的磷酸化。在許多人類腫瘤細胞系中IC50=（37-48 nM）,如HT29,LOX,SKOV3和SKVLB細胞,Camptothecin能夠在納摩爾級別表現(xiàn)出細胞毒性作用。 |
| 激酶實驗 | 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 |
| 細胞實驗 | 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) |
| 別名 | CPT, NSC-100880, (S)-(+)-Camptothecin, 喜樹堿, Campathecin |
| 分子量 | 348.36 |
| 分子式 | C20H16N2O4 |
| CAS No. | 7689-03-4 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 3.48 mg/mL (10 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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