| 供货周期： | 一周 |
| 品牌： | 爱必信 |
| 规格： | ＞98% |
| 货号： | abs812037 |
| CAS号： | 763113-22-0 |
| 公告提醒：爱必信所有产品和服务仅用于科学研究，不用于临床应用及其他用途提供产品和服务（也不为任何个人提供产品和服务）!
抑制剂描述： 产品名称：Olaparib (AZD2281, KU0059436) 产品别名：见爱必信官网 英文别名：Olaparib (AZD2281, KU0059436) 靶点：PARP CAS：763113-22-0 纯度：＞98% 外观：见爱必信官网 保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述： Olaparib (AZD2281, Ku-0059436)是一种选择性的PARP1/2抑制剂，无细胞试验中IC50为5 nM/1 nM，比对Tankyrase-1的作用强300倍。 溶解性：DMSO ：80 mg/mL (184.1 mM) 体外研究： Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 μM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways. 体内研究：Combining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. Olaparib shows great response to Brca1-/-;p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-;p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors.
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