生物活性
MST-312 is a telomerase Inhibitor. Telomeres are nucleoprotein complexes present on the ends of chromosomes, containing DNA segment tandem repeats that shorten with each repetitive cell cycle. Telomere shortening leads to loss of function, resulting in cell senescence and limited survivability. The reverse transcriptase, telomerase, maintains telomere length and function in immortalized cell lines and most cancer cell lines, and telomerase activity is associated with tumorigenesis. Telomere elongation is also believed to be an important contributor to the genomic stability and indefinite self renewal of iPS cells. 1 μM MST-312 was shown to effectively reduce telomere length and inhibit proliferation in U937 cells.
化学数据
分子量 | 380.35 |
分子式 | C20H16N2O6 |
CAS号 | 368449-04-1 |
纯度 | >98% |
溶解性(25°C) | DMSO: ≥20 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 |
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 |
---|
1 mM | 2.6292 mL | 13.1458 mL | 26.2916 mL |
5 mM | 0.5258 mL | 2.6292 mL | 5.2583 mL |
10 mM | 0.2629 mL | 1.3146 mL | 2.6292 mL |