祝贺AbMole成为ChemBridge中国区唯一官方指定合作伙伴!

AZD2281 (Olaparib) 奥拉帕尼

目录号 M1664 所有产品仅供科研使用,严禁用于人或动物的治疗等任何其他用途,不为任何个人提供产品和服务  


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。

AZD2281 (Olaparib)结构式

别名:Olaparib, KU-0059436

包装 价格 库存状态
10mM*1mL 原价 ¥ 570
促销价 ¥ 541.5
中国库存现货
10mg 原价 ¥ 500
促销价 ¥ 475
中国库存现货
50mg 原价 ¥ 1100
促销价 ¥ 1045
中国库存现货
100mg 原价 ¥ 1650
促销价 ¥ 1567.5
中国库存现货
其他规格数量报价?

质量控制及产品安全说明书
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。

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) 0.02 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,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据
分子量 434.46
分子式 C24H23FN4O3
CAS号 763113-22-0
纯度 99.84%
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
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 / Mass 1 mg 5 mg 10 mg
1 mM 2.3017 mL 11.5085 mL 23.0171 mL
5 mM 0.4603 mL 2.3017 mL 4.6034 mL
10 mM 0.2302 mL 1.1509 mL 2.3017 mL
使用AbMole产品发表的文献
客户产品验证及相关生物数据
数据来源 Int J Biol Sci (2018 Oct). Figure 5. Olaparib (Abmole Bioscience, Houston, USA)
方法 IP
细胞系 mice
浓度 100 mg/kg
处理时间 -
实验结果 The overall RTVs (treated vs. non-treated tumors) for mice bearing Brca1-mutant tumor allografts were 60.8% and 62.6% for mice treated with MK-2206 and olaparib, respectively.
数据来源 Int J Biol Sci (2018 Oct). Figure 4. Olaparib (Abmole Bioscience, Houston, USA)
方法 IP
细胞系 mice
浓度 100 mg/kg
处理时间 -
实验结果 In mice co-treated with olaparib and MK-2206, tumor volume was only increased ~1.8-fold at this same time, indicating that these agents exerted a additive effect on tumor growth.
数据来源 Int J Oncol (2015). Figure 4. AZD2281
方法 apoptosis assay
细胞系 HCC‑1428 cells
浓度 2 μM
处理时间 4 day
实验结果 Inhibition of autophagy by knocking down ATG5 also partially inhibited AZD2281-induced apoptosis, suggesting that autophagy contributes to AZD2281-induced cell death in BRCA mutated breast cancer cells.
数据来源 Int J Oncol (2015). Figure 1. AZD2281
方法 Transmission electron microscopy
细胞系 BRCA1 or BRCA2 mutant breast cancer cell lines
浓度 2 μM
处理时间 4 day
实验结果 The growth inhibition effect of AZD2281 was significantly higher in the BRCA wild-type cell lines with BRCA1 allelic loss than in the BRCA wild-type cell line without BRCA1 allelic loss.
参考文献

Synthetic lethality of PARP and NAMPT inhibition in triple-negative breast cancer cells.
Bajrami et al. EMBO Mol Med. 2012 Aug 30. PMID: 22933245.

Clinical trials and future potential of targeted therapy for ovarian cancer.
Itamochi et al. Int J Clin Oncol. 2012 Aug 28. PMID: 22926640.

PI3K inhibition impairs BRCA1/2 expression and sensitizes BRCA proficient triple negative breast cancer to PARP inhibition.
Ibrahim et al. Cancer Discov. 2012 Aug 24. PMID: 22915752.

Cross-platform pathway-based analysis identifies markers of response to the PARP inhibitor olaparib.
Daemen et al. Breast Cancer Res Treat. 2012 Sep;135(2):505-17. PMID: 22875744.

Olaparib , PARP1 inhibitor in ovarian cancer.
Marchetti et al. Expert Opin Investig Drugs. 2012 Jul 13. PMID: 22788971.

  获取最新目录册
Abmole10周年目录册
其他相关的PARP产品
BRCA1-IN-2

BRCA1-IN-2是一种细胞渗透性的BRCA1蛋白-蛋白相互作用(PPI)抑制剂,其IC50值为0.31 μM,Kd值为0.3 μM。

RBN-2397

RBN-2397是一种有效的,具有口服活性的NAD+竞争性PARP7抑制剂,IC50值小于3 nM。

Pamiparib

Pamiparib (BGB-290)是一种有效的PARP1和PARP2选择性抑制剂,对PARP1和PARP2的IC50值分别为0.9 nM和0.5 nM。

BGP-15 2HCl

BGP-15是一种新型的聚(ADP-核糖)聚合酶 PARP 抑制剂,其IC50和Ki值分别为120 μM和57 μM。

Benzamide

Benzamide是一种PARP的抑制剂,其IC50值为3.3 μM。





关键词:AZD2281 (Olaparib), Olaparib, KU-0059436, AZD2281 (Olaparib)供应商, PARP抑制剂, 购买AZD2281 (Olaparib), AZD2281 (Olaparib)结构式

联系我们

Copyright © 2010-2020 AbMole版权所有 沪ICP备16047849号

沪公网安备 31011502012228号

产品仅供实验室人员研究使用,不对个人出售。