生物活性
CUDC-305是一种小分子热休克蛋白HSP90的抑制剂。
化学数据
分子量 | 442.58 |
分子式 | C22H30N6O2S |
CAS号 | 1061318-81-7 |
纯度 | >98% |
溶解性(25°C) | DMSO 10 mM |
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 |
---|
细胞系 | BT474, N87, H1975, H1993, Calu-6 and H460 cells line |
方法 | Cell growth and viability assay. Human cancer cell lines were purchased from American Type Culture Collection and plated at 5,000 to 10,000 per well in 96-well plates with culture medium, as suggested by the provider. The cells were then incubated with compounds at various concentrations for 120 h. Growth inhibition was assessed by ATP content assay using the Perkin-Elmer ATPlite kit. Briefly, a 25-μL cell lysis solution was added to the 50-μL phenol red–free culture medium per well to lyse cells and stabilize ATP. Then 25-μL substrate solutions were added to the wells, and subsequently, luminescence was measured with a TopCount liquid scintillation analyzer (Perkin-Elmer). Values were expressed as a percentage relative to those obtained in untreated controls. IC50 values were calculated using PRISM software (GraphPad Software) with sigmoidal dose-response curve fitting. |
浓度 | 0~900nM |
处理时间 | 120h |
动物实验 |
---|
动物模型 | U87MG glioblastoma tumor models |
配制 | formulated in 30% Captisol |
剂量 | single 160 mg/kg |
给药处理 | oral gavage |
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 | 2.2595 mL | 11.2974 mL | 22.5948 mL |
5 mM | 0.4519 mL | 2.2595 mL | 4.519 mL |
10 mM | 0.2259 mL | 1.1297 mL | 2.2595 mL |