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HA14-1
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。
HA14-1图片
CAS NO:65673-63-4
包装:10mg, 50mg
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍

生物活性

HA14-1是非肽类Bcl-2表面口袋配体,IC50为9 μM。HA14-1 is a small molecule which has the potential of inducing apoptosis in cancerous cells. HA14-1 manifests an antagonistic effect on antiapoptotic protein Bcl-2 and consequently induces cell death in various cancerous cell lines. HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively.P53 pathway to be the probable mechanism of action for the induction of apoptosis in HeLa cell by downregulating the effect of anti-apoptotic proteins suggesting that HA14-1 may provide therapeutic potential for the treatment of human cervical cancer.


化学数据

分子量409.23
分子式C17H17BrN2O5
CAS号65673-63-4
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
细胞系HF1A3, HF4.9 and HF28RA cells
方法Determining the cytotoxic effects of HA14-1 against different FL cell lines by the MTT assay. Briefly, incubating the cells (5000/well) in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, adding the MTT solution to each well. After 4 h incubation at 37 °C, measuring the optical density (OD) by means of 96-well plate reader, with the extraction buffer as a blank. The following formula is used: percentage cell viability = (OD of the experiment samples/OD of the control) ?100. Sigmoidal dose-response curves are fitted to the mean cell viability plotted against log HA14-1 dose and lethal concentration 50% (LC50) values are calculated from the resulting curves using Prism 4.0 softw
浓度~25 μM
处理时间20 h

动物实验
动物模型Female Swiss nude mice bearing BeGBM xenografts
配制Free RPMI 1640-50% DMSO.
剂量400 nM
给药处理Inject at the site of cell injection.

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 mM2.4436 mL12.2181 mL24.4361 mL
5 mM0.4887 mL2.4436 mL4.8872 mL
10 mM0.2444 mL1.2218 mL2.4436 mL