A PARP inhibitor
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Labeled Version(s)
9002700Olaparib-d4
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Olaparib

Item No. 10621

Technical Information
Formal Name
4-[[3-[[4-(cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-1(2H)-phthalazinone
CAS Number
763113-22-0
Synonyms
  • AZD 2281
  • Ku-0059436
Molecular Formula
C24H23FN4O3
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 3 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
279 nm
SMILES
O=C(C1CC1)N2CCN(C(C3=C(F)C=CC(CC(C4=C5C=CC=C4)=NNC5=O)=C3)=O)CC2
InChi Code
InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30)
InChi Key
FDLYAMZZIXQODN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Olaparib is a potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM).1 It can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.1,2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Menear, K.A., Adcock, C., Boulter, R., et al4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A novel bioavailable inhibitor of Poly(ADP-ribose) polymerase-1. J. Med. Chem. 51(20), 6581-6591 (2008).

    2. Yuan, Y., Liao, Y.M., Hsueh, C.T., et alNovel targeted therapeutics: Inhibitors of MDM2, ALK and PARP. J. Hematol. Oncol. 4(16), 1-14 (2011).

    3. Plummer, R. Poly(ADP-ribose) polymerase inhibition: A new direction for BRCA and triple-negative breast cancer? Breast Cancer Res. 13(4), 1-6 (2011).

    4. Javle, M., and Curtin, N.J. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther. Adv. Med. Oncol. 3(6), 257-267 (2011).

    Product Citations

    Gardell, S.J., Hopf, M., Khan, A., et alBoosting NAD+ with a small molecule that activates NAMPT. Nat. Commun. 10(1), 3241 (2019).