2. Cell Cycle/DNA Damage Epigenetics Autophagy
  3. PARP Autophagy Mitophagy
  4. Olaparib

オラパリブ  (Synonyms: Olaparib; AZD-2281; KU-0059436)

製品番号: HY-10162 純度: 99.98%
COA 取扱説明書

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Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.

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Olaparib 構造式

オラパリブ 構造式

CAS 番号 : 763113-22-0

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 在庫あり
Solution
10 mM * 1 mL in DMSO USD 66 在庫あり
Solid
5 mg USD 38 在庫あり
10 mg USD 60 在庫あり
20 mg USD 70 在庫あり
50 mg USD 84 在庫あり
100 mg USD 108 在庫あり
200 mg USD 144 在庫あり
500 mg USD 216 在庫あり
1 g USD 300 在庫あり
2 g USD 540 在庫あり
5 g   お問い合わせ  
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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 206 publication(s) in Google Scholar

Other Forms of Olaparib:

オラパリブ 関連抗体

Top Publications Citing Use of Products

顧客検証

Proliferation Assay
WB
IHC

    Olaparib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430.  [Abstract]

    Immunoblots (IB) are done to detect γH2AX and DNA repair proteins, Ku80 and RAD51 using UAB-PA4 or UAB-PA16 tumors harvested from mice 24 h following final treatment. Quantitation by densitometry of results is shown below each IB image.

    Olaparib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 May;43:225-237.  [Abstract]

    Representative images of immunohistochemical staining for proteins as indicated in A2780 xenografted tumors (n=6 per treatment group) treated with Olaparib and PD 0332991 either as single-agents or in combination for 4 days.

    Olaparib purchased from MedChemExpress. Usage Cited in: J Biomed Sci. 2019 Feb 4;26(1):14.   [Abstract]

    Inhibition of NFBD1 results in defective γ-H2AX foci formation after Olaparib exposure, cells are exposed to Olaparib for 24 h, and the γ-H2AX positive cells are determined by FCM

    Olaparib purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2019 Jan;17(1):42-53.  [Abstract]

    Combination of RAD001 with Olaparib (left panel) and AZD2014 with Olaparib (right panel) activates the RIPK1 Ser 166 phosphorylation in Clone A and SF-539 cells respectively.

    Olaparib purchased from MedChemExpress. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.  [Abstract]

    CCDN1 protein level in tumor samples of different treatment groups (control, scrambled shRNA treated, Olaparib + scrambled shRNA treated, or Olaparib + CCND1-shRNA treated) are analyzed by western blot.

    Olaparib purchased from MedChemExpress. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.  [Abstract]

    The expression of CCND1mRNA and cyclin D1 protein level in A2780 and SKOV3 cells is analyzed by western blot after Olaparib treatment at IC50 concentrations.

    Olaparib purchased from MedChemExpress. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.  [Abstract]

    Immunohistochemistry of RAD51 and γ-H2AX in samples of SKOV3 tumors. Representative sections are taken from tumor tissue of control, scrambled shRNA treated, Olaparib + scrambled shRNA treated, or Olaparib + CCND1-shRNA treated mice.

    Olaparib purchased from MedChemExpress. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.  [Abstract]

    Immunohistochemistry for CCND1 is performed in tumor samples in the treatment of compounds (control, scrambled shRNA treated, Olaparib + scrambled shRNA treated, or Olaparib + CCND1-shRNA treated).

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

    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 MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688.  [Abstract]

    EW8 and TC71 cells are treated with Olaparib (5 μM) or U0126 (5 μM) for 24 hours and then protein synthesis is assessed using puromycin labeling.

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

    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 MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867.  [Abstract]

    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 MedChemExpress. Usage Cited in: Int J Mol Sci. 2016 Feb 24;17(3):272.  [Abstract]

    The effect of 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).

    PARP アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].

    IC50 & Target[1]

    PARP-2

    1 nM (IC50)

    PARP-1

    5 nM (IC50)

    tankyrase-1

    1.5 μM (IC50)

    Autophagy

     

    Mitophagy

     

    体外実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    オラパリブ 関連抗体
    体内実験

    Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with NSC 362856 (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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    434.46

    分子式

    C24H23FN4O3
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (230.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    DMF : 50 mg/mL (115.09 mM; Need ultrasonic)

    Ethanol : 3.12 mg/mL (7.18 mM; ultrasonic and warming and heat to 60°C)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    Concentration (final)

    C2

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 10 mg/mL (23.02 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 10 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 5 mg/mL (11.51 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (46.03 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
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    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
    %
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    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.98%

    COA (250 KB) HNMR (221 KB) LCMS (120 KB) Elemental Analysis Report (108 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMF / DMSO 1 mM 2.3017 mL 11.5085 mL 23.0171 mL 57.5427 mL
    5 mM 0.4603 mL 2.3017 mL 4.6034 mL 11.5085 mL
    DMF / DMSO 10 mM 0.2302 mL 1.1509 mL 2.3017 mL 5.7543 mL
    15 mM 0.1534 mL 0.7672 mL 1.5345 mL 3.8362 mL
    20 mM 0.1151 mL 0.5754 mL 1.1509 mL 2.8771 mL
    25 mM 0.0921 mL 0.4603 mL 0.9207 mL 2.3017 mL
    30 mM 0.0767 mL 0.3836 mL 0.7672 mL 1.9181 mL
    40 mM 0.0575 mL 0.2877 mL 0.5754 mL 1.4386 mL
    50 mM 0.0460 mL 0.2302 mL 0.4603 mL 1.1509 mL
    60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9590 mL
    80 mM 0.0288 mL 0.1439 mL 0.2877 mL 0.7193 mL
    100 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5754 mL
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    Olaparib Related Classifications

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Olaparib763113-22-0AZD2281 KU0059436AZD 2281AZD-2281KU0059436KU 0059436KU-0059436PARPAutophagyMitophagypoly ADP ribose polymerase Mitochondrial AutophagyorallyPARP1PARP2Inhibitorinhibitorinhibit

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