Olaparib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、特异性、口服活性的 PARP 抑制剂，对 PARP1 和 PARP2 的 IC50 分别为 5 和 1 nM。

A potent, specific, and orally active PARP inhibitor with IC50 of 5 and 1 nM for PARP1 and PARP2, respectively; displays 300-fold selectivity over tankyrase (TNKS-1 IC50=1.5 uM); shows standalone activity against BRCA1-deficient breast cancer cell lines; regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin.Ovarian Cancer Approved(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.

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AZD2281 | KU-0059436 | KU0059436 | | AZD 2281

Cell Cycle/DNA Damage

PARP

PARP1|PARP2

Cancer

Ovarian Cancer

763113-22-0

434.4628

C24H23FN4O3

>98% (HPLC)

DMSO: 29 mg/mL

O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(C4CC4)=O)CC3)=O)=C2)C5=C1C=CC=C5

1(2H)-Phthalazinone, 4-[[3-[[4-(cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-

(-20℃)

With Ice Pack

≥ 2 years