Olaparib (AZD2281, KU0059436)是选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，其对PARP1/2的作用比对Tankyrase-1效果高300倍。在BRCA突变的细胞中，Olaparib可以显著地诱导线粒体自噬相关的细胞自噬。
| CAS No. | 763113-22-0 |
| 生物活性 | Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. |
| 分子式 | C24H23FN4O3 |
| 分子量 | 434.46 |
| 储存条件 | Powder -20℃ 3 years |
| 溶解性数据 | DMF : 50 mg/mL (115.09 mM; Need ultrasonic) DMSO : ≥ 33.33 mg/mL (76.72 mM) Ethanol : 3.12 mg/mL (7.18 mM; ultrasonic and warming and heat to 60°C) |
| 体内研究 | Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with NSC 362856 (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors. |
| 体外研究 | Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC50 for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30−100 nM. |
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| 纯度及产品资料 | 98% |
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