1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  2. PARP
    Autophagy

Olaparib (Synonyms: AZD2281; KU-0059436; KU0059436; AZD-2281; KU0059436; AZD 2281)

Cat. No.: HY-10162 Purity: 99.71%
Data Sheet SDS Handling Instructions

Olaparib is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1 and PARP-2, respectively.

For research use only. We do not sell to patients.
Olaparib Chemical Structure

Olaparib Chemical Structure

CAS No. : 763113-22-0

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10 mM * 1 mL in DMSO $55 In-stock
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Customer Review

Top Publications Citing Use of Products

    Olaparib purchased from MCE. Usage Cited in: Int J Mol Sci. 2016 Feb 24;17(3):272.

    The effect of Cisplatin and AZD2281 on the protein expression of xenografted HSC-2 tumors. Relative band intensity of western blot data is normalized by the expression level of β-actin; The proteins analyzed are PARP-1 (poly(ADP-ribose) polymerase-1).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Olaparib is a potent PARP inhibitor with IC50 of 5 and 1 nM for PARP-1 and PARP-2, respectively.

    IC50 & Target

    IC50: 5/1 nM (PARP-1/2)[1]

    In Vitro

    Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC50 for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30−100 nM[1].

    In Vivo

    Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with Temozolomide (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out[1]. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors[2].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.3017 mL 11.5085 mL 23.0171 mL
    5 mM 0.4603 mL 2.3017 mL 4.6034 mL
    10 mM 0.2302 mL 1.1509 mL 2.3017 mL
    Kinase Assay
    [1]

    This assay determined the ability of Olaparib to inhibit PARP-1 enzyme activity. PARP-2 activity inhibition is measured by using a variation of the PARP-1 assay in which PARP-2 protein (recombinant) is bound down by a PARP-2 specific antibody in a 96-well white-walled plate. PARP-2 activity is measured following 3H-NAD+ DNA additions. After washing, scintillant is added to measure 3H-incorporated ribosylations. For tankyrase-1, an AlphaScreen assay is developed in which HIS-tagged recombinant TANK-1 protein is incubated with biotinylated NAD+ in a 384-well ProxiPlate assay. Alpha beads are added to bind the HIS and biotin tags to create a proximity signal, whereas the inhibition of TANK-1 activity is directly proportional to the loss of this signal. All experiments are repeated at least three times[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Olaparib is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    The PF50 value is the potentiation factor, which is calculated as the ratio of the IC50 of the control growth with alkylating agent methylmethane sulfonate (MMS) divided by the IC50 of the MMS combined with the PARP inhibitor. HeLa B cells are used, and Olaparib is tested at a fixed 200 nM concentration for screening with MMS. For the testing of Olaparib on the SW620 colorectal cell line, the concentrations that are used are 1, 3, 10, 100 and 300 nM. Cell growth is assessed by the use of the sulforhodamine B (SRB) assay[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Olaparib is prepared in PBS (containing 10% DMSO and 10% 2-hydroxy-propyl-β-cyclodextrin) (Mice)[2].

    Mice[2]
    Mice bearing 220-250 mm3 tumors are randomized into 4 treatment groups (n=5): A; vehicle control (10% DMSO in PBS/10% 2-hydroxy-propyl-β-cyclodextrin daily for 5 days by oral gavage), B; Olaparib (50 mg/kg daily for 5 days by oral gavage), C; 10 Gy fractionated radiotherapy (2 Gy daily for 5 days), D; Olaparib and 10 Gy (5×2 Gy) fractionated radiotherapy (with olaparib given 30 min prior to each daily 2 Gy dose of radiation). Tumor volume measurements are determined daily until they reached 1000 mm3. The number of days for each individual tumor to quadruple in size from the start of the treatment (relative tumor volume×4; RTV4) is calculated for the individual tumors in each group. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    M.Wt

    434.46

    Formula

    C₂₄H₂₃FN₄O₃

    CAS No.

    763113-22-0

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 29 mg/mL; in vivo: dissolved in DMSO (31.25 mg/mL) and then diluted with PBS (DMSO: PBS=1:9)

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.71%

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    Inquiry Information

    Product Name:
    Olaparib
    Cat. No.:
    HY-10162
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