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

Olaparib (Synonyms: 奥拉帕尼; AZD2281; KU0059436)

目录号: HY-10162 纯度: 99.98%
产品使用指南

Olaparib (AZD2281; KU0059436) 是一种口服有效的 PARP 抑制剂,抑制 PARP-1PARP-2IC50 分别为 5 和 1 nM。Olaparib 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

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Olaparib Chemical Structure <

Olaparib Chemical Structure

CAS No. : 763113-22-0

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 110 篇科研文献

    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 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 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: 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. 2019 Jan;17(1):42-53.

    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 MCE. Usage Cited in: Mol Cancer Ther. 2018 Dec;17(12):2676-2688.

    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 MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.

    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 MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.

    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 MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.

    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 MCE. Usage Cited in: Gynecol Oncol. 2019 Jan;152(1):157-165.

    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 MCE. Usage Cited in: J Biomed Sci. 2019 Feb 4;26(1):14. 

    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 MCE. Usage Cited in: EBioMedicine. 2019 May;43:225-237.

    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 MCE. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430.

    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.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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

     

    体外研究
    (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].

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

    体内研究
    (In Vivo)

    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].

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

    Clinical Trial
    分子量

    434.46

    Formula

    C24H23FN4O3

    CAS 号
    中文名称

    奥拉帕尼;奥拉帕利

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 100 mg/mL (230.17 mM; Need ultrasonic)

    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)

    配制储备液
    浓度 溶剂体积 质量 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
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

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

    • 2.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

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

    • 3.

      请依序添加每种溶剂: 10% DMF    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    • 4.

      请依序添加每种溶剂: 10% DMF    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    • 5.

      请依序添加每种溶剂: 10% DMF    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    • 6.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.75 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 7.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 8.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

      此方案可获得 ≥ 2.08 mg/mL (4.79 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 9.

      请依序添加每种溶剂: 1% DMSO    99% saline

      Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    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.

    参考文献

    纯度: 99.98%

    • 摩尔计算器

    • 稀释计算器

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    质量   浓度   体积   分子量 *
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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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