Olaparib Basic information
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Product Name: |
Olaparib |
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Synonyms: |
1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)Methyl]-2-fluorobenzoyl]piperazin;Olaparid AZD2281;4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one;4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]Methyl]-1(2H)-phthalazinone;KU 59436;AZD2281(olaparib)/AZD-2281;AZD2281(olaparib);4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one |
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CAS: |
763113-22-0 |
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MF: |
C24H23FN4O3 |
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MW: |
434.46 |
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EINECS: |
642-941-5 |
Olaparib Chemical Properties
| density | 1.43 |
| storage temp. | -20°C |
| solubility | Soluble in DMSO (up to 33 mg/ml) or in Ethanol (up to 1.7 mg/ml) |
| pka | 12.07±0.40(Predicted) |
| form | solid |
| color | Off-White |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
Olaparib Usage And Synthesis
| Description | Olaparib, marketed by AstraZeneca under the brand name Lynparza , was approved in the USA in December 2014 as a targeted, single-agent therapy for the treatment of germline BRCA-mediated advanced ovarian cancer.Olaparib, originally developed by KuDOS pharmaceuticals and later by AstraZeneca, functions as a poly ADP ribose polymerase inhibitor and has been specifically approved for patients who have received three or more treatments of chemotherapy. In clinical trials, the drug prolonged progression- free survival for patients suffering from platinum-sensitive recurrent serous ovarian cancer. Olaparib is also currently in various phases of investigation for treatment of breast, gastric, prostate, pancreatic and non-small cell lung cancer. |
| Chemical Properties | White Solid |
| Uses | Olaparib is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Olaparib has been shown to induce significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Recent studies show that Olaparib increases radiosensitivity of a lung tumor xenograft, making it a potential candidate for use in combination with radiotherapy. |
| Definition | ChEBI: Olaparib is a member of the class of N-acylpiperazines obtained by formal condensation of the carboxy group of 2-fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid with the free amino group of N-(cyclpropylcarbonyl)piperazine; used to treat advanced ovarian cancer. It has a role as an antineoplastic agent, an EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor and an apoptosis inducer. It is a N-acylpiperazine, a member of cyclopropanes, a member of monofluorobenzenes and a member of phthalazines. |
Oraparib is a chemotherapeutic agent used to treat recurrent or advanced ovarian cancer and metastatic breast cancer in patients with specific mutations and a history of previous chemotherapy. Olaparib, marketed under the Lynparza brand as oral tablets, was initially designated as a maintenance therapy or monotherapy for treating adult patients with recurrent epithelial ovarian cancer, fallopian tube cancer, or primary peritoneal cancer.
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