Olaparib (AZD2281, Ku-0059436) [763113-22-0]
Referencia A4154-10mg
embalaje : 10mg
Marca : APExBIO Technology
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Olaparib (AZD2281, Ku-0059436)
Olaparib (AZD2281, Ku-0059436; CAS 763113-22-0) is a selective inhibitor of poly(ADP-ribose) polymerase-1 and -2 (PARP-1/2). By targeting PARP enzymes involved in DNA repair, Olaparib specifically inhibits the proliferation of BRCA-deficient tumor cell lines and enhances radiosensitivity in experimental tumor models. In xenograft mouse models of non-small cell lung carcinoma (NSCLC), Olaparib has been shown to elevate radiation sensitivity and improve tumor perfusion. The compound is widely utilized in studies focused on DNA damage responses, tumor radiosensitization, and targeted therapy strategies for BRCA-associated cancers.
Reference
Joana M. Senra, Brian A. Telfer, Kim E. Cherry, Cian M. McCrudden, David G. Hirst, Mark J. O’Connor, Stephen R. Wedge, and Ian J. Stratford. Inhibition of poly(ADP-ribose) polymerase-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft. Mol Cancer Ther. 2011; 10(10): 1949-1958
Bastiaan Evers, Rinske Drost, Eva Schut, Michiel Bruin, Eline vab der Burg, Patrick W.B. Derksen, Henne Holstege, Xiaoling Liu, Ellen van Drunen, H. Berna Beverloo, Graeme C. M. Smith, Niall M. B. Martin, Alan Lau, Mark J. O’Connor, and Jos Jonkers. Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and Cisplatin. Clin Cancer Res 2008; 14:3916-3925
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| Storage | Store at -20°C |
| M.Wt | 434.46 |
| Cas No. | 763113-22-0 |
| Formula | C24H23FN4O3 |
| Synonyms | AZD 2281,AZD-2281 |
| Solubility | ≥21.72 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one |
| Canonical SMILES | O=C(C1CC1)N(CC1)CCN1C(c(cc(CC(c1c2cccc1)=NNC2=O)cc1)c1F)=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment: [1] | |
| Cell lines | Normal LCL cells ATM-null LCL cells |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reaction Conditions | 10 μM, 1 hour |
| Applications | The sensitivity of cells to olaparib is mediated by absence of Ataxia Telangiectasia Mutated (ATM) activity. Immunoblot analysis revealed that in ATM wild-type LCLs, but not ATM null LCLs, phosphorylation of the ATM-dependent targets ATM S1981 and SMC1 S966 was induced in a dose-dependent manner by olaparib. |
| Animal experiment: [1] | |
| Animal models | Granta-519–engrafted NOD/SCID mice |
| Dosage form | Intraperitoneal injection, 50 mg/kg/d, for 14 days |
| Applications | Analysis of the percentage of human CD45 staining by FACS analysis revealed a significant reduction in the percentage of Granta-519 cells in the bone marrow and a trend toward reduced tumor cell load in the spleen of mice treated with olaparib compared with those receiving vehicle alone. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Weston V J, Oldreive C E, Skowronska A, et al. The PARP inhibitor olaparib induces significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Blood, 2010, 116(22): 4578-4587. | |
| Olaparib (AZD2281, KU0059436) is a potent inhibitor of PARP1 and PARP2 with IC50 of 5 and 1 nM, respectively. | ||||||
| Targets | PARP1 | PARP2 | ||||
| IC50 | 5 nM | 1 nM | ||||
Quality Control & MSDS
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