151519-02-7
151519-02-7 结构式
基本信息
中文别名
化合物 T16543 英文别名
PIRONETIN2H-Pyran-2-one, 5-ethyl-5,6-dihydro-6-[(2R,3S,4R,5S,7E)-2-hydroxy-4-methoxy-3,5-dimethyl-7-nonen-1-yl]-, (5R,6R)-
物理化学性质
熔点75-77 °C
沸点473.1±40.0 °C(Predicted)
密度0.993±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度Dichloromethane: soluble; DMSO: soluble; Ethanol: soluble
酸度系数(pKa)14.28±0.20(Predicted)
形态固体
颜色Colorless to off-white
常见问题列表
生物活性
Pironetin 是从链霉菌属物种分离的 α/β 不饱和内酯。Pironetin 与 α-tubulin 结合，是微管聚合的有效抑制剂，具有细胞周期停滞和抗肿瘤活性。靶点
Microtubule
体外研究
Pironetin (20-100 ng/mL; 24 hours; 3Y1 cells) treatment arrests the cell cycle progression at G2/M in 3Y1 cells.
Pironetin (1-10000 ng/mL; 3 days; HeLa, A2780 and K-NRK cells) treatment inhibits the cell proliferation.
IC
50
values against these cell lines are almost 10 ng/mL.
Cell Cycle Analysis
| Cell Line: | 3Y1 cells |
| Concentration: | 20 ng/mL, 50 ng/mL, 100 ng/mL |
| Incubation Time: | 24 hours |
| Result: | Arrested the cell cycle progression at G2/M in3Y1 cells. |
Cell Proliferation Assay
| Cell Line: | HeLa, A2780 and K-NRK cells |
| Concentration: | 1 ng/mL, 10 ng/mL, 100 ng/mL, 1000 ng/mL and 10000 ng/mL |
| Incubation Time: | 3 days |
| Result: | Inhibited the cell proliferation. |
体内研究
Pironetin (0.78-6.25 mg/kg; intraperitoneal injection; daily; for 5 days; female CDF1-SLC mice) treatment shows a moderate antitumor effect, however, a severe weight loss is observed as a side effect.
| Animal Model: | Female CDF1-SLC mice (10 weeks) injected with P388 murine leukemia cells |
| Dosage: | 0.78 mg/kg, 1.56 mg/kg, 3.13 mg/kg, 6.25 mg/kg |
| Administration: | Intraperitoneal injection; daily; for 5 days |
| Result: | Showed a moderate antitumor effect. |