Olaparib
Olaparib is an inhibitor of poly(ADP-ribose) polymerase (PARP 1/2) that prevents DNA repair. Olaparib displays benefit in clinical trials of BRCA mutation-harboring ovarian and breast cancers as well as prostate, pancreatic, and non-small cell lung cancers (NSCLC). In animal models with ovarian cancer xenografts, olaparib increases apoptosis and decreases proliferation to inhibit tumor growth.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18950725
| Cas No. |
763113-22-0 |
|---|---|
| Purity |
≥98% |
| Formula |
C24H23FN4O3 |
| Formula Wt. |
434.47 |
| IUPAC Name |
4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one |
| Synonym |
AZD2281, KU-0059436 |
| Solubility |
DMSO (10 mg/ml), DMF (3 mg/ml) |
| Appearance |
White to off white powder |
Lee JM, Ledermann JA, Kohn EC. PARP Inhibitors for BRCA1/2 mutation-associated and BRCA-like malignancies. Ann Oncol. 2013 Nov 12. [Epub ahead of print]. PMID: 24225019.
Olaparib Enters Phase III Clinical Testing. Cancer Discov. 2013 Nov;3(11):1210. PMID: 24203936.
Postel-Vinay S, Bajrami I, Friboulet L, et al. A high-throughput screen identifies PARP1/2 inhibitors as a potential therapy for ERCC1-deficient non-small cell lung cancer. Oncogene. 2013 Nov 21;32(47):5377-87. PMID: 23934192.
Kortmann U, McAlpine JN, Xue H, et al. Tumor growth inhibition by olaparib in BRCA2 germline-mutated patient-derived ovarian cancer tissue xenografts. Clin Cancer Res. 2011 Feb 15;17(4):783-91. PMID: 21097693.
