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Olaparib

CAS No. : 763113-22-0

MCE 站：Olaparib

产品活性：Olaparib (AZD2281; KU0059436) 是一种口服有效的 PARP 抑制剂，抑制 PARP-1 和 PARP-2 的 IC₅₀ 分别为 5 和 1 nM。Olaparib 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Autophagy

作用靶点：PARP  |  Autophagy  |  Mitophagy

In Vitro: 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.

In Vivo: 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.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Epigenetics Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  CNS-Penetrant Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Targeted Therapy Drug Library   |  3-Methyladenine  |  Doxorubicin hydrochloride  |  SB 203580  |  Deferoxamine mesylate  |  Dexamethasone  |  Metformin hydrochloride  |  U0126-EtOH  |  Etoposide  |  AICAR  |  Brefeldin A  |  Resveratrol  |  XAV-939  |  Quercetin  |  Melatonin  |  Curcumin  |  Valproic acid  |  Sunitinib  |  Tanespimycin  |  Hemin  |  Simvastatin  |  Tripterin  |  Ivermectin  |  Aspirin  |  Kaempferol  |  Oxidopamine hydrobromide  |  Betulinic acid  |  Rucaparib  |  Salinomycin  |  Sulfosuccinimidyl oleate sodium

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