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AZD2281(Olaparib)
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。
AZD2281(Olaparib)图片
CAS NO:763113-22-0
包装:10mg, 25mg, 50mg, 100mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mM*1mL in DMSO电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
Olaparib, KU-0059436
产品介绍

生物活性

Olaparib (AZD2281, Ku-0059436)是一种选择性的PARP1/2抑制剂,IC50为5 nM/1 nM,比对Tankyrase-1的作用强300倍。Olaparib是PARP抑制剂,也作用于BRCA1或BRCA2突变。Olaparib对端锚(聚合)酶-1作用效果不大,IC50值大于。Olaparib浓度为30-100 nM作用于SW620细胞,使PARP-1失活。


化学数据

分子量434.46
分子式C24H23FN4O3
CAS号763113-22-0
纯度99.86%
溶解性(25°C)DMSO 80 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SW620 colorectal cell line
方法Potentiation of MMS Cytotoxicity by 47 Determined by the Use of Sulforhodamine B Cell Growth Assays. SW620 cells were seeded in 96-well plates and were left to attach overnight. Cells were preincubated with vehicle control (DMSO) or with a single concentration of KU-0059436 (1, 3, 10, 30, 100 or 300 nM) for 1 h before the addition of increasing concentrations of MMS. Cells were incubated in the presence of each drug combination for 4 days before cell growth was quantified by the use of an SRB assay.44 Data were calculated from triplicate wells as the mean percentage of cell growth relative to KU-0059436-only wells, and (SE and IC50 were calculated by the use of XL-FIT 4 software. SW620 cells showed<24% growth inhibition (>76% cell growth) when only KU-0059436 was used at concentrations below 300 nM (data not shown).
浓度1, 3, 10, 100 and 300 nM
处理时间4 days

动物实验
动物模型mouse bearing SW620 xenografted tumors
配制methylcellulose/PBS
剂量10 mg/kg once daily for 5 consecutive days
给药处理orally

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 mM2.3017 mL11.5085 mL23.0171 mL
5 mM0.4603 mL2.3017 mL4.6034 mL
10 mM0.2302 mL1.1509 mL2.3017 mL