生物活性
Plicamycin光神霉素A是一种DNA结合、抗肿瘤和神经保护性的抗生素。Plicamycin光神霉素A也是选择性的Sp1抑制剂,它结合富含GC的DNA序列,取代了Sp1转录因子与癌基因启动子的结合,抑制了它们的表达。Plicamycin(10-200 nM)可以使肿瘤细胞对TRAIL诱导的细胞凋亡敏感并被用于在许多不同的癌症模型中选择性靶向肿瘤细胞。
In vivo, the antitumorigenic activity of Plicamycin (0.2 mg/kg/day) is determined in a xenograft model and observed reduction in tumor volume and weight. No significant mouse body weight loss is observed in Plicamycin-treatment groups, indicating that Plicamycin-associated toxicity is minimal. Plicamycin also increases TUNEL-positive cells in tumor xenografts.
化学数据
分子量 | 1085.15 |
分子式 | C52H76O24 |
CAS号 | 18378-89-7 |
纯度 | USP,85%,900mcg/mg |
溶解性(25°C) | DMSO 14 mg/mL |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | HEp-2 cells and KB cells |
方法 | HEp-2 cells and KB cells are cultured in DMEM 100 U/mL each of Penicillin and Streptomycin and 10% FBS for HEp-2 cells and 5% FBS for KB in a humidified atmosphere containing 5% CO2 at 37°C. Equal numbers of cells are seeded and allowed to attach. At 50-60% confluence, cells are treated with DMSO or indicated concentrations of Plicamycin (50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells). After treatment, 30 μL MTS solution is added to each well and cells are incubated for 2 h at 37°C. MTS solution is analyzed using a microplate reader at 490 nm and 690 nm. |
浓度 | 50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells |
处理时间 | - |
动物实验 |
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动物模型 | Female nude mice |
配制 | - |
剂量 | 0.2 mg/kg/day, three times per week for 29 days |
给药处理 | i.p. |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 0.9215 mL | 4.6077 mL | 9.2153 mL |
5 mM | 0.1843 mL | 0.9215 mL | 1.8431 mL |
10 mM | 0.0922 mL | 0.4608 mL | 0.9215 mL |