生物活性
FH535 antagonizes β-Catenin/Tcf–mediated transcription, and inhibits recruitment of the coactivators GRIP1 and β-catenin to PPARδ and PPARγ. FH535 increases cigarette smoke condensate cytotoxicity, and causes changes in β-catenin and EGR-1 signaling. FH535 inhibits β-catenin and GRIP1 recruitment to PPARγ and δ. FH535 Exhibits antiproliferative effects in transformed colon, lung and liver cancer cell lines.
化学数据
分子量 | 361.20 |
分子式 | C13H10Cl2N2O4S |
CAS号 | 108409-83-2 |
纯度 | >98.5% |
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 |
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 | HCT116, SW48, RKO, LoVo, COLO205, IEC6, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b, Huh7, Fibroblasts |
方法 | Determining cell viability by the modified 3H-thymidine incorporation assay. Briefly, plating cells in 96-well microplates for 24 h and treating in triplicate with various concentrations of the test compound. After 48 h of compound exposure, incubating the cells for an additional 48 h in compound-free medium. Then incubating the cells in medium containing 3H-thymidine for 24 h, washing and mixing with the scintillant in the 96-well plate. Counting Individual wells with a 96-well scintillation counter and calculating the LC50. |
浓度 | 30 μM |
处理时间 | 48 hours |
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
以下数据基于半岛bd体育手机客户端
分子量,对于特殊半岛bd体育手机客户端
,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 | 2.7685 mL | 13.8427 mL | 27.6855 mL |
5 mM | 0.5537 mL | 2.7685 mL | 5.5371 mL |
10 mM | 0.2769 mL | 1.3843 mL | 2.7685 mL |