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%
COA 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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10 mM * 1 mL in DMSO ¥567
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5 mg ¥321
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10 mg ¥515
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20 mg ¥750
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50 mg ¥1300
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100 mg ¥1980
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200 mg ¥2950
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500 mg ¥4950
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1 g ¥6950
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2 g ¥9950
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Customer Review

Other Forms of Olaparib:

MCE 顾客使用本产品发表的 195 篇科研文献

WB
Proliferation Assay
IHC

    Olaparib purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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).
    • 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) 是 PARP-1 和 PARP-2 的个位数纳摩尔抑制剂,对 BRCA1 缺陷型乳腺癌细胞系显示出独立的活性。将 Olaparib 应用于 SW620 细胞裂解物,确定 PARP-1 抑制的 IC50 约为 6 nM,PARP-1 活性的总消融浓度为 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)

    携带 SW620 异种移植肿瘤的动物用 Olaparib (10 mg/kg,口服,每天 1 次,共 5 天) 与 NSC 362856 (TMZ) (50 mg/kg,口服) 联合处理抗肿瘤[1]。Olaparib 增加在 DWC 模型中建立的 Calu-6 肿瘤的血管灌注。Olaparib (50 mg/kg,口服) 作为单一药物或与放疗联合使用导致 Calu-6 肿瘤的荧光强度增加[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
    性状

    固体

    颜色

    White to yellow

    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (230.17 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    DMF 中的溶解度 : 50 mg/mL (115.09 mM; 超声助溶)

    Ethanol 中的溶解度 : 3.12 mg/mL (7.18 mM; 超声助溶 (<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
    查看完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    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

    • 方案 一

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

      Solubility: 10 mg/mL (23.02 mM); 悬浊液; 超声助溶

      此方案可获得 10 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 100.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      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); 澄清溶液

    以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

    • 方案 一

      请依序添加每种溶剂: 0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (46.03 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.98%

    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

    完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 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
    Help & FAQs
    • Do most proteins show cross-species activity?

      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.

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    产品名称:
    Olaparib
    目录号:
    HY-10162
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