AZD2281 (olaparib) is phthalazinone-based PARP inhibitor with a potencies of 5 nM and 1 nM for PARP1 and PARP2, respectively. It has been shown to be efficacious in the treatment of breast cancer tumors with BRCA mutations. Specifically, BRCA2 deficient tumor cells showed the strongest differential growth inhibition upon treatment with AZD2281 when compared to BRCA2-proficient cells. [1]AZD2281 has been studied in combination therapies with platinum-based drugs and taxanes; specifically, synergistic toxicity in BRCA2-deficient cells has been shown with cisplatin. [1] AZD2281 has been shown to be a radiosensitizer in the treatment of NSCLC cells. [2]
Technical information:
| Chemical Formula: | C24H23FN4O3 | |
| CAS #: | 763113-22-0(937799-91-2) | |
| Molecular Weight: | 434.46 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AZD2281, AZD-2281, Olaparib, KU-0059436 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Evers et al., Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and cisplatin. Clin Cancer Res 2008, 14(12), 3916-3925. Pubmed ID:18559613 |
| 2. | Senra et al., Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft. Mol Cancer Ther. 2011, 10(10), 1949-1958. Pubmed ID:21825006 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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