Plicamycin 目录号M9262
化学数据
分子量分子式CAS号储存条件
1085.15C52H76O2418378-89-73年 -20°C 粉末状
溶解性（25°C）
DMSO 14 mg/mLWater
Ethanol 7 mg/mL
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.
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）细胞实验细胞系方法
HEp-2 cells and KB cells
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.
浓度处理时间
50, 100, and 200 nM for HEp-2 cells; 20, 40, and 80 nM for KB cells-
动物实验动物模型配制剂量给药处理
Female nude mice-0.2 mg/kg/day, three times per week for 29 daysi.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
重量 (kg)体表面积 (m2)Km系数
0.020.0073
大鼠0.150.0256
动物B的Km系数动物A的Km系数
兔1.80.1512
豚鼠0.40.058
仓鼠0.080.025
狗100.520
动物A (mg/kg) = 动物B (mg/kg) ×
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 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 / Mass1 mM5 mM10 mM
1 mg0.9215 mL0.1843 mL0.0922 mL
5 mg4.6077 mL0.9215 mL0.4608 mL
10 mg9.2153 mL1.8431 mL0.9215 mL
参考文献
Modulation of specificity protein 1 by mithramycin A as a novel therapeutic strategy for cervical cancer.Choi ES, et al. Sci Rep. 2014 Nov 24;4:7162. PMID: 25418289.
所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务。抑制剂化合物库CCK-8 / 蛋白酶抑制剂Cocktail
AbMole中国
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