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    Olaparib (AZD2281; KU0059436)
    Olaparib (AZD2281; KU0059436)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0300
    CAS #: 763113-22-0Purity ≥98%

    Description: Olaparib (formerly also known as AZD-2281; KU-59436; KU0059436; trade name Lynparza) is a potent, novel and orally bioavailable small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential anticancer activity. It inhibits PARP with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. It has potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. Olaparib was approved in 2014 by FDA for treating advanced ovarian cancer.

    References: J Med Chem. 2008 Oct 23;51(20):6581-91; Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84.

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    Molecular Weight (MW)434.46
    FormulaC24H23FN4O3
    CAS No.763113-22-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (197.9 mM)          
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O: 5 mg/mL
    Synonyms

    AZD2281, Ku-0059436; AZD2281; AZD-2281; AZD 2281; KU59436; KU-59436; KU 59436; KU0059436; KU-0059436; KU 0059436; Olaparib. trade name Lynparza

    Chemical Name: 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one

    SMILES Code: O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(C4CC4)=O)CC3)=O)=C2)C5=C1C=CC=C5


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    In Vitro

    In vitro activity: Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 μM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways.


    Kinase Assay: To columns 1 through 10, 1 μL of Olaparib (in DMSO) is added, and 1 μL DMSO only is added to the positive (POS) and negative (NEG) control wells (columns 11 and 12, respectively) of a pretreated FlashPlate. PARP-1 is diluted 1:40 in buffer (buffer B: 10% glycerol (v/v), 25 mM HEPES, 12.5 mM MgCl2,50 mM KCl, 1 mM DTT, 0.01% NP-40 (v/v), pH 7.6) and 40 μL added to all 96 wells (final PARP-1 concentration in the assay is ~1 ng/μL). The plate is sealed and shaken at RT for 15 min. Following this, 10 μL of positive reaction mix (0.2 ng/μL of double-stranded oligonucleotide [M3/M4] DNA per well, 5 μM of NAD+ final assay concentration, and 0.075 μCi 3H-NAD+ per well) is added to the appropriate wells (columns 1-11). The negative reaction mix, lacking the DNA oligonucleotide, is added to column 12 (with the mean negative control value used as the background). The plate is resealed and shaken for a further 60 min at RT to allow the reaction to continue. Then, 50 μL of ice-cold acetic acid (30%) is added to each well to stop the reaction, and the plate is sealed and shaken for a further 60 min at RT. Tritiated signal bound to the FlashPlate is then determined in counts per minute (CPM) using the TopCount plate reader.


    Cell Assay: The cytotoxicity of Olaparib is measured by clonogenic assay. Olaparib is dissolved in DMSO and diluted by culture media before use. The cells (Breast cancer cell lines including SW620 colon, A2780 ovarian, HCC1937, Hs578T, MDA-MB-231, MDA-MB-436, and T47D) are seeded in six well plates and left to attach overnight. Then Olaparib is added at various concentrations and the cells are incubated for 7-14 days. After that the surviving colonies are counted for calculating the IC50.

    In VivoCombining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. Olaparib shows great response to Brca1-/-;p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-;p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors.
    Animal modelGranta-519–engrafted NOD/SCID mice
    Formulation & DosageDissolved in 50 mg/mL stocks in DMSO with 10% 2-hydroxyl-propyl-β-cyclodextrine/PBS;  50 mg/kg;  i.p. injection
    References

    J Med Chem. 2008 Oct 23;51(20):6581-91; Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84; Blood. 2010 Nov 25;116(22):4578-87.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Olaparib (AZD2281, Ku-0059436)

    AZD2281 treatment induces DNA damage-associated foci and caspase 3-mediated apoptosis. Proc Natl Acad Sci U S A. 2008 Nov 4; 105(44): 17079–17084.
     

    Olaparib (AZD2281, Ku-0059436)

    Combination of AZD2281 with carboplatin and cisplatin prolongs recurrence-free survival and overall survival.
     

    Olaparib (AZD2281, Ku-0059436)

    Increased expression of Abcb1a and Abcb1b is associated with AZD2281 resistance in vivo.


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