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Olaparib

カタログ番号 T3015   CAS 763113-22-0
別名: AZD2281, KU0059436

Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.

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Olaparib, CAS 763113-22-0
パッケージサイズ 在庫状況 単価(税別) キャンペーン価格
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5 mg 在庫あり ¥ 7,500 6,000
10 mg 在庫あり ¥ 11,000 9,000
50 mg 在庫あり ¥ 16,000 13,000
100 mg 在庫あり ¥ 21,000 17,000
200 mg 在庫あり ¥ 27,500 22,000
500 mg 在庫あり ¥ 41,000 33,000
1 g 在庫あり ¥ 57,000 46,000
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生物学的特性に関する説明
化学的特性
保存条件 & 溶解度情報
説明 Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.
ターゲット&IC50 PARP2:1 nM (cell free), PARP1:5 nM (cell free)
In vitro METHODS: Human cervical cancer cells SiHa and ME180 were treated with Olaparib (5-10 µM) and cisplatin (1-30 µM) for 72 h. Cell growth inhibition was detected by MTT.
RESULTS: Olaparib and cisplatin co-treatment showed significant cell growth inhibition compared to cells treated with a single drug. [1]
METHODS: Human endometrial cancer cells HEC-6 and HEC-6-PTEN were treated with Olaparib (10 μM) for 72 h. The cell cycle was analyzed by Flow Cytometry.
RESULTS: Olaparib induced a significant increase in the sub-G1 population of HEC-6 and HEC-6-PTEN cells. [2]
METHODS: Chicken lymphoma cells DT40 were treated with Olaparib (0.01-10 μM) for 30 min, and the expression levels of target proteins were detected by Western Blot.
RESULTS: Olaparib dose-dependently inhibited the expression level of PARylation and the activation of PARP. [3]
In vivo METHODS: To detect anti-tumor activity in vivo, Olaparib (10 mg/kg) and TMZ (50 mg/kg) were orally administered to mice bearing human colorectal cancer tumor SW620 once daily for five days.
RESULTS: Significant suppression of tumor volume was observed in the TMZ plus Olaparib combination treatment group compared to the TMZ group alone. [4]
METHODS: To investigate the therapeutic effects of Olaparib on asthma, Olaparib (1-10 mg/kg) was administered intraperitoneally once daily for three days to an OVA-based asthmatic C57BL/6 mouse model.
RESULTS: Olaparib significantly reduced airway eosinophilia, mucus production, and hyperresponsiveness. The protective effects of Olaparib were associated with inhibition of the Th2 cytokines eotaxin, IL-4, IL-5, IL-6, IL-13, and M-CSF, as well as ovalbumin-specific IgE, and an increase in the Th1 cytokine IFN-γ. Olaparib is a potential candidate for clinical trials in human asthma. [5]
キナーゼ試験 This assay determined the ability of test compounds to inhibit PARP-1 enzyme activity. The method that was used was as reported. We measured PARP-2 activity inhibition by using a variation of the PARP-1 assay in which PARP-2 protein (recombinant) was bound down by a PARP-2 specific antibody in a 96-well white-walled plate. PARP-2 activity was measured following 3H-NAD+ DNA additions. After washing, scintillant was added to measure 3 H-incorporated ribosylations. For tankyrase-1, an AlphaScreen assay was developed in which HIS-tagged recombinant TANK-1 protein was incubated with biotinylated NAD+ in a 384-well ProxiPlate assay. Alpha beads were added to bind the HIS and biotin tags to create a proximity signal, whereas the inhibition of TANK-1 activity was directly proportional to the loss of this signal. All experiments were repeated at least three times [1].
細胞研究 HSC-2, Ca9-22, and SAS oral carcinoma cells were seeded in 24-well plates at a density of 2 × 104 cells/well. After overnight incubation, the culture medium was replaced with fresh medium containing various concentrations of PARP inhibitor AZD228 or cisplatin. After 24 h of treatment, the number of viable cells was assessed using an MTT assay as reported previously. Briefly, one-tenth of the fluid volume of 5 mg/mL MTT in RPMI-1640 medium was added to each well, followed by incubation for 4 h at 37 °C. After incubation, the medium was carefully removed and an adequate volume of 0.1 N HCl in isopropanol was added to each well and the resultant formazan crystals was dissolved. Absorbance was determined at 570 nm by microplate reader in 96-well assay plates. All experiments were performed in triplicate [2].
動物実験 Once the tumor diameter had reached 7 mm, the mice were randomly assigned to the following groups: (a) control (200 μL saline); (b) cisplatin (2 mg/kg per body weight, dissolved in 200 μL sterilized water); (c) AZD2281 (25 mg/kg per body weight, dissolved in 200 μL sterilized water); or (d) combination (both cisplatin and AZD2281). The chemicals were administered intraperitoneally every three days, five times. Although AZD2281 is administered orally in the clinic, intraperitoneal injection was recommended by the manufacturer because of easier manipulation and the ethical constraints associated with oral gavage administration to mice. Tumor size and body weight were measured at the time of administration. The tumor volume was calculated using following equation. Tumor volume = verticality × width × height × 0.5236. Three days after the last administration, all surviving mice were sacrificed [2].
別名 AZD2281, KU0059436
分子量 434.46
分子式 C24H23FN4O3
CAS No. 763113-22-0

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 80 mg/mL (184.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

参考文献

1. Prasad CB, et al. Olaparib modulates DNA repair efficiency, sensitizes cervical cancer cells to cisplatin and exhibits anti-metastatic property. Sci Rep. 2017 Oct 9;7(1):12876. 2. Miyasaka A, et al. Anti-tumor activity of olaparib, a poly (ADP-ribose) polymerase (PARP) inhibitor, in cultured endometrial carcinoma cells. BMC Cancer. 2014 Mar 13;14:179. 3. Murai J, et al. Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors. Cancer Res. 2012 Nov 1;72(21):5588-99. 4. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91. 5. Ghonim MA, et al. PARP inhibition by olaparib or gene knockout blocks asthma-like manifestation in mice by modulating CD4(+) T cell function. J Transl Med. 2015 Jul 14;13:225.

引用文献

1. Long X, Dai A, Huang T, et al.Simultaneous Delivery of Dual Inhibitors of DNA Damage Repair Sensitizes Pancreatic Cancer Response to Irreversible Electroporation.ACS nano.2023 2. Valentini E, Di Martile M, Brignone M, et al.Bcl-2 family inhibitors sensitize human cancer models to therapy.Cell Death & Disease.2023, 14(7): 441. 3. Pan X, Zhang W, Wang L, et al.KLF12 transcriptionally regulates PD‐L1 expression in non‐small cell lung cancer.Molecular Oncology.2023 4. Zhao J, Xu J, Wu M, et al.LncRNA H19 Regulates Breast Cancer DNA Damage Response and Sensitivity to PARP Inhibitors via Binding to ILF2.International Journal of Molecular Sciences.2023, 24(11): 9157. 5. Yu L, Zhou D, Zhang G, et al. Co‐occurrence of BAP1 and SF3B1 mutations in uveal melanoma induces cellular senescence. Molecular Oncology.. 2022, 16(3): 607-629. 6. Malka M M, Eberle J, Niedermayer K, et al. Dual PARP and RAD51 Inhibitory Drug Conjugates Show Synergistic and Selective Effects on Breast Cancer Cells. Biomolecules. 2021, 11(7): 981. 7. Du T, Zhang Z, Zhou J, et al. A Novel PARP Inhibitor YHP-836 For the Treatment of BRCA-Deficiency Cancers. Frontiers in pharmacology. 2022, 13. 8. Dai W, Wu J, Peng X, et al. CDK12 orchestrates super‐enhancer‐associated CCDC137 transcription to direct hepatic metastasis in colorectal cancer. Clinical and Translational Medicine. 2022, 12(10): e1087. 9. Guffanti F, Alvisi M F, Anastasia A, et al. Basal expression of RAD51 foci predicts olaparib response in patient-derived ovarian cancer xenografts. British Journal of Cancer. 2021: 1-9. 10. Wu Y, Wu T, Hu X, et al. Proguanil synergistically sensitizes ovarian cancer cells to olaparib by increasing DNA damage and inducing apoptosis. International Journal of Medical Sciences. 2022, 19(2): 233-241.
隠し

関連化合物ライブラリー

この製品は下記化合物ライブラリに含まれています:
EMA Approved Drug Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Inhibitor Library DNA Damage & Repair Compound Library Anti-Breast Cancer Compound Library

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同一標的の関連化合物
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投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください
投与量
mg/kg
動物の平均体重
g
動物あたりの投与量
ul
動物数
溶媒の組成を入力してください
% DMSO
%
% Tween 80
% ddH2O
計算する リセット

計算器

モル濃度計算機
希釈計算機
再構成計算
分子量計算機
=
X
X

モル度計算機では以下の計算が可能です

  • 既知の体積と濃度の溶液を調製するために必要な化合物の質量
  • 質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
  • 特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度
参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか?
[分子量(MW)]の欄に[197.13]と入力してください
[濃度]ボックスに10と入力し、正しい単位(millimolar)を選択します
[容量]ボックスに10と入力し、正しい単位(milliliter)を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

X
=
X

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2&V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか?
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度(開始)ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度(終了)ボックスに50を入力し正しい単位(millimolar)を選択してください
体積(終了)ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積(開始)ボックスに表示されます。

=
/

バイアルを再構成するのに必要な溶媒の量を計算する.

再構成計算機を使えば、バイアルを再構成するための試薬の量をすぐに計算することができます.
試薬の質量と目標濃度を入力するだけで計算します。

g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント:化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量(分子量)を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量(分子量)とは、物質の1分子の質量であり、統一された原子質量単位(u)で表されます。(1uは炭素12の1原子の質量の1/12に等しい)
モル質量(molar weight)とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Olaparib 763113-22-0 Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Mitophagy PARP AZD2281 Mitochondrial Autophagy inhibit orally Inhibitor PARP1 KU0059436 poly ADP ribose polymerase PARP2 KU 0059436 AZD-2281 AZD 2281 KU-0059436 inhibitor