Name: Olaparib (AZD2281, Ku-0059436)
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Olaparib (4-(3-4-fluorophenyl) methyl-1(2H)-one), as known as AZD2281 or KU0059436, is a novel, selective and potent inhibitor of both poly adenosine diphosphate-ribose polymeras-1 (PARP-1) and poly adenosine diphosphate-ribose polymeras-2 (PARP-2). Having been successfully used in the treatment of tumors harboring BRCA mutations, olaparib strongly inhibits the growth of BRCA2-deficient mouse mannary tumor cell lines demonstrating cytotoxicity. In previous researches treating non-small cell lung carcinoma (NSCLC), olaparib increased the radiation sensitivity of NSCLC cells, grown as xenografts in nude mice, following radiation and increased vascular perfusion in Calu-6 tumors established in a dorsal window chamber (DWC) model.
- Properties
  - Alternative Name
    
    AZD 2281,AZD-2281; 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one
    
    CAS Number
    
    763113-22-0
    
    Molecular Formula
    
    C24H23FN4O3
    
    Molecular Weight
    
    434.46
    
    Purity
    
    99.64%
    
    Solubility
    
    ≥21.72 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Leonie Schürmann, Lena Schumacher, et al. "Inhibition of the DSB repair protein RAD51 potentiates the cytotoxic efficacy of doxorubicin via promoting apoptosis-related death pathways." Cancer Lett. 2021 Nov 1;520:361-373. PMID:34389435
    2. Asha Sinha, Sachin Katyal, et al. "PARP-DNA trapping ability of PARP inhibitors jeopardizes astrocyte viability: Implications for CNS disease therapeutics." Neuropharmacology. 2021 Apr 1;187:108502. PMID:33631119
    3. Phoebe McCrorie, Jatin Mistry, et al. "Etoposide and olaparib polymer-coated nanoparticles within a bioadhesive sprayable hydrogel for post-surgical localised delivery to brain tumours." Eur J Pharm Biopharm. 2020 Oct 14;S0939-6411(20)30305-2. PMID:33068736
    4. Kim DS, Camacho CV, et al. "Activation of PARP-1 by snoRNAs Controls Ribosome Biogenesis and Cell Growth via the RNA Helicase DDX21." Mol Cell. 2019 Jul 9. pii: S1097-2765(19)30476-9. PMID:31351877
    5. Singatulina AS, Hamon L, et al. "PARP-1 Activation Directs FUS to DNA Damage Sites to Form PARG-Reversible Compartments Enriched in Damaged DNA." Cell Rep. 2019 May 7;27(6):1809-1821.e5. PMID:31067465
    6. Kong X, Cruz GMS, et al. "Biphasic recruitment of TRF2 to DNA damage sites promotes non-sister chromatid homologous recombination repair." J Cell Sci. 2018 Dec 5;131(23). pii: jcs219311. PMID:30404833
    7. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID:30038713
    8. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID:29988031
    9. Coyle JP, Rinaldi RJ, et al."Reduced oxygen tension culturing conditionally alters toxicogenic response of differentiated H9c2 cardiomyoblasts to acrolein." Toxicol Mech Methods. 2018 Mar 22:1-39. PMID:29564938
    10. Kong X, Cruz GMS, et al. "Laser Microirradiation to Study In Vivo Cellular Responses to Simple and Complex DNA Damage." J Vis Exp. 2018 Jan 1;(131). PMID:29443023
    11. Iniguez AB, Stolte B, et al. "EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma." Cancer Cell. 2018 Feb 12;33(2):202-216.e6. PMID:29358035
    12. Xiangduo Kong,Gladys Mae Saquilabon Cruz,et al."Biphasic recruitment of TRF2 to DNA damage sites promotes non-sister chromatid homologous recombination repair."bioRxiv. April 20.
    13. Mackay DR, Howa AC, et al. "Nup153 and Nup50 promote recruitment of 53BP1 to DNA repair foci by antagonizing BRCA1-dependent events." J Cell Sci.2017 Oct 1;130(19):3347-3359. PMID:28751496
    14. Skvarova Kramarzova K, Osborn MJ, et al. "CRISPR/Cas9-Mediated Correction of the FANCD1 Gene in Primary Patient Cells." Int J Mol Sci. 2017 Jun 14;18(6). pii: E1269. PMID:28613254
    15. Gao Y, Li C, et al. "SSRP1 Cooperates with PARP and XRCC1 to Facilitate Single-Strand DNA Break Repair by Chromatin Priming." Cancer Res.2017 May 15;77(10):2674-2685. PMID:28416484
    16. Raymond D, Harbison, Ph.D, et al. "The Inﬂuence of Oxygen Tension and Glycolytic and Citric Acid Cycle Substrates in Acroleininduced Cellular Injury in the Diﬀerentiated H9c2 Cardiac Cell Model."University of South Florida. 2016 Nov.
    17. Höhn A, Krüger K, et al. "Distinct mechanisms contribute to acquired cisplatin resistance of urothelial carcinoma cells." Oncotarget. 2016 Jul 5;7(27):41320-41335. PMID:27191498
    18. Cruz, Gladys Mae Saquilabon, et al. "Femtosecond near-infrared laser microirradiation reveals a crucial role for PARP signaling on factor assemblies at DNA damage sites." Nucleic acids research (2015): gkv976. PMID:26424850

Olaparib (AZD2281, Ku-0059436)

Olaparib (AZD2281, Ku-0059436)

Background

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