生物活性
ML323是一种高效、选择性的USP1-UAF1抑制剂,IC50为76 nM。分别。
化学数据
分子量 | 384.48 |
分子式 | C23H24N6 |
CAS号 | 1572414-83-5 |
纯度 | >98% |
溶解性(25°C) | DMSO |
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 | H596 cells |
方法 | For the colony-forming assay, seeding cells at a density of 300–500 cells per well in six-well plates and growing overnight.Then treating cells with ML323 alone, cisplatin alone or a combination of cisplatin and ML323 (1:1 or 1:4) at the indicated concentrations. Treating cells with an equal volume of DMSO and usinf saline as control. After 48 h of treatment, adding fresh growth medium, and incubating cells for an additional 5-10 d to allow for colony formation. For UV combination treatment, treating the cells with ML323 at the indicated concentrations or an equal volume of DMSO. After 48 h, removing the medium , and irradiating cells at 254 nm at the indicated dosage. Adding fresh growth medium , and incubating the cells for an additional 5-10 d to allow for colony formation. The cells without UV irradiation but treated with ML323 or an equal volume of DMSO are used as controls and designated as 100%. After the formation of the colonies, fixing cells with methanol and stained with 0.5% crystal violet. Colonies consisting of >50 cells are scored. The number of colonies is determined from triplicate plates. The dose-response curves are generated using GraphPad Prism and analyzed by using CalcuSyn to calculate the combination index, which is determined for the fraction of cells affected after the addition of fixed ratios of cisplatin and the USP1-UAF1 inhibitor. |
浓度 | ~30 μM |
处理时间 | 7-12 days |
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 | 2.6009 mL | 13.0046 mL | 26.0092 mL |
5 mM | 0.5202 mL | 2.6009 mL | 5.2018 mL |
10 mM | 0.2601 mL | 1.3005 mL | 2.6009 mL |