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Belinostat
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。
Belinostat图片
CAS NO:414864-00-9
包装:5mg, 10mg, 50mg, 100mg, 200mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mM*1mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品名称
PXD101, PX105684
产品介绍

生物活性

Belinostat (PXD101)是一种新型的HDAC抑制剂,IC50为27 nM,对抵抗Cisplatin的肿瘤有效。Belinostat抑制肿瘤细胞生长(包括A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3,及HS852),IC50为0.2到0.66 μM。Belinostat 作用于A2780/cp70 和2780AD细胞时活性很低, 这两个细胞是抗cisplatin和doxorubicin的A2780细胞衍生的。Belinostat通过PARP分裂和组蛋白H3/H4的乙酰化而诱导细胞凋亡。


化学数据

分子量318.35
分子式C15H14N2O4S
CAS号414864-00-9
纯度99.52%
溶解性(25°C)DMSO 60 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A2780, A2780/cp70, CALU-3, MCF7, PC3, HS852, HT29 and HCT116 cell lines
方法Cytotoxicity Assay.
Drug sensitivity was determined by a clonogenic assay (13). Briefly, cells were plated in 5 ml of medium at a density of 8 × 104 cells/25 cm2 flask and allowed to attach and grow for 48 h. Cells were exposed to drug (five concentrations from 0.016 to 10 μM) for 24 h. The medium was removed, and 1 ml of trypsin/EDTA was added to each flask. Once the cells had detached, 1 ml of medium was added, the cells were resuspended, and those from the control untreated flask were counted. Cells were diluted and plated into 6-cm Petri dishes (three per flask) at a density of 500-2000 cells/dish depending on the cell line. Cells from the drug-treated flasks were diluted and plated as for the control flasks. Dishes were incubated for 10–15 days at 37°C. Cells were washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 (mean ± SE of three experiments) defined as the concentration of drug required to reduce the number of colonies to 50% of that of the control untreated cells.
浓度0.016 ~ 10 μM
处理时间24 h

动物实验
动物模型A2780, A2780/cp70 and HCT116 tumor-bearing mice model
配制dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10%
剂量a single injection of 40 mg/kg
给药处理i.p.

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 mM3.1412 mL15.706 mL31.412 mL
5 mM0.6282 mL3.1412 mL6.2824 mL
10 mM0.3141 mL1.5706 mL3.1412 mL