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

Olaparib (Synonyms: AZD2281; KU0059436)

Cat. No.: HY-10162 Purity: 99.71%
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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
Estimated Time of Arrival: December 31
100 mg USD 108 In-stock
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200 mg USD 144 In-stock
Estimated Time of Arrival: December 31
500 mg USD 216 In-stock
Estimated Time of Arrival: December 31
1 g USD 300 In-stock
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2 g USD 540 In-stock
Estimated Time of Arrival: December 31
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Customer Review

    Olaparib purchased from MCE. Usage Cited in: Oncogene. 2018 Jan 18;37(3):341-351.

    PTEN-deficient endometrioid endometrial cancer cell lines are treated with drugs as indicated for 24 h. Phosphorylated AKT, S6RP and 4EBP1 proteins and cleaved PARP are detected by western blot. Vinculin served as a loading control.

    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).

    Olaparib purchased from MCE. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.

    In vivo dosing of BGJ398 at 30mg/kg achieves target inhibition measured by pFrs2 and pErk levels.

    Olaparib purchased from MCE. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.

    MEK inhibitor Trametinib (GSK1120212) achieves target inhibition at 3mg/kg.

    Olaparib purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867.

    PARP1 inhibition is lethal to MPM cells. Colony formation assays of clonal cell survival with continuous Niraparib or Olaparib, both at 3 uM. a H2452 BPA1-mutant MPM cells exposed to Niraparib. b HMeso01A BAP1-mutant MPM cells exposed to Niraparib. cHMeso01A BAP1-mutant MPM cells exposed to Olaparib. d CRL-2081 BAP1 wild-type MPM cells exposed to Olaparib. e CRL-2081 BAP1 wild-type MPM cells exposed to Niraparib. f Dose response of H2452 BPA1-mutant MPM cells exposed to varying concentrations of

    Olaparib purchased from MCE. Usage Cited in: Eur J Pharmacol. 2017 Nov 15;815:147-155.

    Shown are GFPu fluorescent images of the GFPu-HEK293 cells treated with CuSO4 (Cu, 20 μM), HK (20 μM), HK-Cu (HC, 20 μM), or Velcade (Vel, 100 nM).

    Olaparib purchased from MCE. Usage Cited in: Cancer Discov. 2018 Mar;8(3):354-369.

    At 50mg/kg, Crizotinib inhibits MET phosphorylation and downstream signaling pathway activation.

    Olaparib purchased from MCE. Usage Cited in: Oncol Rep. 2018 Apr;39(4):1747-1756.

    The effect of Olaparib on protein expression. Western blot assays of MUS81 and MCM2 expression levels in A2780 and SKOV3 cells after treatment with 5 μM Olaparib compared with a blank control.

    Olaparib purchased from MCE. Usage Cited in: Mol Cancer Res. 2018 Sep 10.

    Combination of Everolimus with Olaparib (left panel) and AZD2014 with Olaparib (right panel) activates the RIPK1 Ser 166 phosphorylation in Clone A and SF-539 cells respectively.
    • 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[1]

    PARP-2

    1 nM (IC50)

    PARP-1

    5 nM (IC50)

    tankyrase-1

    1.5 μM (IC50)

    Autophagy

     

    Mitophagy

     

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : 29 mg/mL (66.75 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO  90% saline

      Solubility: ≥ 3.1 mg/mL (7.14 mM); Clear solution

    References
    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]

    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]

    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
    Molecular Weight

    434.46

    Formula

    C₂₄H₂₃FN₄O₃

    CAS No.

    763113-22-0

    SMILES

    O=C(C1=CC(CC(C2=C3C=CC=C2)=NNC3=O)=CC=C1F)N4CCN(C(C5CC5)=O)CC4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.71%

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

    Cat. No.: HY-10162