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LAQ824
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LAQ824图片
CAS NO:404951-53-7
包装:10mg, 50mg
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品名称
NVP-LAQ824
产品介绍

生物活性

LAQ824 (Dacinostat)是新型HDAC抑制剂,IC50为32 nM,且激活p21启动子。在体外, LAQ824抑制 H1299细胞裂解液中的人HDAC活性, IC50 为32 nM。此外, LAQ824通过激活p21 启动子,也激活编码p21 细胞周期抑制剂的基因表达,最大启动子活性 (AC50)为50%时,浓度为0.30 μM。 处理72小时后, LAQ824抑制 H1299(一种非小细胞肺癌细胞)和HCT116(一种结肠癌细胞)细胞生长,IC50分别为0.15 μM和 0.01 μM, LAQ824的抗增殖效果选择性作用于肿瘤细胞系。


化学数据

分子量379.459
分子式C22H25N3O3
CAS号404951-53-7
纯度>95%
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
细胞系HCT116, H1299, PC-3, DU145 and MDA435 cells
方法Monolayer Growth Inhibition Assay. Cell proliferation was measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay) as described previously (29) . The CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay was performed according to the manufacturer’s protocol. The average background value (treatment with medium alone) was subtracted from each experimental well; triplicate values were averaged for each compound dilution. The following formulas were used to calculate the percentage of growth: The “% Growth” was plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.
浓度0~10 μM
处理时间72 hr

动物实验
动物模型HCT116 cells tumor-bearing mice
配制dissolved in DMSO to create a stock solution, which was further diluted just before dosing with D5W to a final DMSO concentration of 10%.
剂量once daily, 5 days/week, for a total of 15 doses.
给药处理i.v. injection into the tail vein

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)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
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 / Mass1 mg5 mg10 mg
1 mM2.6353 mL13.1767 mL26.3533 mL
5 mM0.5271 mL2.6353 mL5.2707 mL
10 mM0.2635 mL1.3177 mL2.6353 mL