生物活性
Tubacin是一种高效的,选择性的,可逆的,细胞通透性的HDAC6抑制剂,IC50为4 nM。
化学数据
分子量 | 721.86 |
分子式 | C41H43N3O7S |
CAS号 | 537049-40-4 |
纯度 | 100.00% |
溶解性(25°C) | DMSO 90 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 | ALL cells and normal T lymphocytes |
方法 | Growth inhibition assay The inhibitory effect of tubacin on ALL cells and normal T lymphocytes was assessed by colorimetric assay, 3-(4,5-dimethylthiazol-e-yl)- 2,5-diphenyl tetrazolium bromide (MTT; Sigma). Only active mitochondria dehydrogenase enzymes can perform cleavage of a tetrazolium ring, and therefore the amount of purple formazan generated by cells with a drug was compared with the amount of formazan produced from non-treated cells. Absorbance readings at a wavelength of 550 nm were taken on a spectrophotometer (Titertek Multiskan MCC Type 341). Cells from 72 h cultures were incubated with 10 μL of 5 mg/mL MTT for 2 h, followed by 100 μL isopropanol that contained 0.1 N HCl. Normal T lymphocytes were incubated with MTT for 30–37 min. All experiments were performed in triplicate. |
浓度 | 0, 0.5, 1, 1.5, 2, 2.5μM |
处理时间 | 72 h |
动物实验 |
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动物模型 | Xenograft system of primary leukemia samples |
配制 | saline |
剂量 | 50 mg/kg/day |
给药处理 | intraperitoneally |
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 | 1.3853 mL | 6.9266 mL | 13.8531 mL |
5 mM | 0.2771 mL | 1.3853 mL | 2.7706 mL |
10 mM | 0.1385 mL | 0.6927 mL | 1.3853 mL |