奥拉帕尼

奥拉帕尼，Olaparib，AZD2281, Ku-0059436，PARP抑制剂。更多视频请关注视频号【艾维缔】。哔哩哔哩【IVDSHOW】。抖音【军哥聊表观】。

关键词

奥拉帕尼

所属分类

抑制剂

目录号

A4154

获取报价

IC50和靶点

生物活性描述	Olaparib (AZD2281, KU0059436)是一种有效的PARP1/2抑制剂，IC50值分别为5 nM和1 nM。.
靶点	PARP1	PARP2
生物活性数据	5 nM	1 nM

参考文献：
Joana M. Senra, Brian A. Telfer, Kim E. Cherry, Cian M. McCrudden, David G. Hirst, Mark J. O’Connor, Stephen R. Wedge, and Ian J. Stratford. Inhibition of poly(ADP-ribose) polymerase-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft. Mol Cancer Ther. 2011; 10(10): 1949-1958
Bastiaan Evers, Rinske Drost, Eva Schut, Michiel Bruin, Eline vab der Burg, Patrick W. B. Derksen, Henne Holstege, Xiaoling Liu, Ellen van Drunen, H. Berna Beverloo, Graeme C. M. Smith, Niall M. B. Martin, Alan Lau, Mark J. O’Connor, and Jos Jonkers. Selective inhibition of BRCA2-deficient mammary tumor cell growth by AZD2281 and Cisplatin. Clin Cancer Res 2008; 14:3916-3925

产品组分

内容	型号	规格	储存温度
奥拉帕尼	A4154-01	10mg	-20°C
奥拉帕尼	A4154-02	100mg	-20°C
奥拉帕尼	A4154-03	500mg	-20°C
操作手册	1	1	常温

文件资源

营销中心
注意事项

保存建议厂家推荐蓝冰运输。当您收到产品后，按照说明书建议保存于-20°C。
FAQ
1. Eleonora Ghisoni, Fabrizio Benedetti, et al. "Myeloid cell networks govern re-establishment of original immune landscapes in recurrent ovarian cancer." Cancer Cell. 2025 Jul 22:S1535-6108(25)00276-4 PMID: 40749672

2. QIAN LI, SHUNPENG ZHU, et al. "SIK2 inhibitor SIC-19 enhances the sensitivity of PARP inhibitors in triple-negative breast cancers and pancreatic cancers." Oncol Res. 2025 Jun 26;33(7):1757–1767 PMID: 40612876

3. Maria V Sukhanova, Rashid O Anarbaev, et al. "Biologically Relevant Polyamines, Divalent Metal Cations, and Structure of Poly(ADP-Ribose) All Control Microphase Separation of FUS with Poly(ADP-Ribosyl)ated PARP1." Biology and Life Sciences. 03 October 2024

4. Hannah L Mackay, Helen R Stone, et al. "USP50 suppresses alternative RecQ helicase use and deleterious DNA2 activity during replication." Nat Commun. 2024 Sep 16;15(1):8102 PMID: 39284827

5. Maria V Sukhanova, Rashid O Anarbaev, et al. "Divalent and multivalent cations control liquid-like assembly of poly (ADP-ribosyl) ated PARP1 into multimolecular associates in vitro." Commun Biol. 2024 Sep 15;7(1):1148 PMID: 39278937

6. Yinan Jiang, Shuting Huang, et al. "Targeting the Cdc2‐like kinase 2 for overcoming platinum resistance in ovarian cancer." MedComm (2020). 2024 Apr 13;5(4):e537. PMID: 38617434

7. Apoorva Uboveja, Zhentai Huang, et al. "αKG-mediated carnitine synthesis promotes homologous recombination via histone acetylation." bioRxiv. 2024 Feb 11:2024.02.06.578742 PMID: 38370789

8. Andrew N. Blackford, et al. "BLM and BRCA1-BARD1 coordinate complementary mechanisms of joint DNA molecule resolution." Mol Cell. 2024 Feb 15;84(4):640-658.e10. PMID: 38266639

9. Seema Khattri Bhandari. "Effect of Ligase I deficiency on replication fork and chromatin." University of New Mexico. March 21, 2023.

10. Judit Jimenez-Sainz, Joshua Mathew, et al. "BRCA2 BRC missense variants disrupt RAD51-dependent DNA repair." Elife. 2022 Sep 13;11:e79183. PMID: 36098506

11. Yinyin Xie, Yannan Zhang, et al. "The coupling of mitoproteolysis and oxidative phosphorylation enables tracking of an active mitochondrial state through MitoTimer fluorescence." Redox Biol. 2022 Oct;56:102447. PMID: 36027677

12. Leonie Schürmann, Lena Schumacher, et al. "Inhibition of the DSB repair protein RAD51 potentiates the cytotoxic efficacy of doxorubicin via promoting apoptosis-related death pathways." Cancer Lett. 2021 Nov 1;520:361-373. PMID: 34389435

13. Fujiao Nie, Jiazhao Yan, et al. "Effect of Shuangdan Mingmu capsule, a Chinese herbal formula, on oxidative stress-induced apoptosis of pericytes through PARP/GAPDH pathway." BMC Complement Med Ther. 2021 Apr 10;21(1):118. PMID: 33838689

14. Asha Sinha, Sachin Katyal, et al. "PARP-DNA trapping ability of PARP inhibitors jeopardizes astrocyte viability: Implications for CNS disease therapeutics." Neuropharmacology. 2021 Apr 1;187:108502. PMID: 33631119

15. Phoebe McCrorie, Jatin Mistry, et al. "Etoposide and olaparib polymer-coated nanoparticles within a bioadhesive sprayable hydrogel for post-surgical localised delivery to brain tumours." Eur J Pharm Biopharm. 2020 Oct 14;S0939-6411(20)30305-2. PMID: 33068736

16. Kim DS, Camacho CV, et al. "Activation of PARP-1 by snoRNAs Controls Ribosome Biogenesis and Cell Growth via the RNA Helicase DDX21." Mol Cell. 2019 Jul 9. pii: S1097-2765(19)30476-9. PMID: 31351877

17. Singatulina AS, Hamon L, et al. "PARP-1 Activation Directs FUS to DNA Damage Sites to Form PARG-Reversible Compartments Enriched in Damaged DNA." Cell Rep. 2019 May 7;27(6):1809-1821.e5. PMID: 31067465

18. Kong X, Cruz GMS, et al. "Biphasic recruitment of TRF2 to DNA damage sites promotes non-sister chromatid homologous recombination repair." J Cell Sci. 2018 Dec 5;131(23). pii: jcs219311. PMID: 30404833

19. Cheriyan VT, Alsaab H, et al. "A CARP-1 functional mimetic compound is synergistic with BRAF-targeting in non-small cell lung cancers." Oncotarget. 2018 Jul 3;9(51):29680-29697. PMID: 30038713

20. Li N, Yang L, et al. "BET bromodomain inhibitor JQ1 preferentially suppresses EBV-positive nasopharyngeal carcinoma cells partially through repressing c-Myc." Cell Death Dis. 2018 Jul 9;9(7):761. PMID: 29988031

21. Coyle JP, Rinaldi RJ, et al."Reduced oxygen tension culturing conditionally alters toxicogenic response of differentiated H9c2 cardiomyoblasts to acrolein." Toxicol Mech Methods. 2018 Mar 22:1-39. PMID: 29564938

22. Kong X, Cruz GMS, et al. "Laser Microirradiation to Study In Vivo Cellular Responses to Simple and Complex DNA Damage." J Vis Exp. 2018 Jan 1;(131). PMID: 29443023

23. Iniguez AB, Stolte B, et al. "EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma." Cancer Cell. 2018 Feb 12;33(2):202-216.e6. PMID: 29358035

24. Xiangduo Kong,Gladys Mae Saquilabon Cruz,et al."Biphasic recruitment of TRF2 to DNA damage sites promotes non-sister chromatid homologous recombination repair."bioRxiv. April 20.

25. Mackay DR, Howa AC, et al. "Nup153 and Nup50 promote recruitment of 53BP1 to DNA repair foci by antagonizing BRCA1-dependent events." J Cell Sci.2017 Oct 1;130(19):3347-3359.

26. Skvarova Kramarzova K, Osborn MJ, et al. "CRISPR/Cas9-Mediated Correction of the FANCD1 Gene in Primary Patient Cells." Int J Mol Sci. 2017 Jun 14;18(6). pii: E1269.

27. Gao Y, Li C, et al. "SSRP1 Cooperates with PARP and XRCC1 to Facilitate Single-Strand DNA Break Repair by Chromatin Priming." Cancer Res.2017 May 15;77(10):2674-2685.

28. Raymond D, Harbison, Ph.D, et al. "The Inﬂuence of Oxygen Tension and Glycolytic and Citric Acid Cycle Substrates in Acroleininduced Cellular Injury in the Diﬀerentiated H9c2 Cardiac Cell Model."University of South Florida. 2016 Nov.

29. Höhn A, Krüger K, et al. "Distinct mechanisms contribute to acquired cisplatin resistance of urothelial carcinoma cells." Oncotarget. 2016 Jul 5;7(27):41320-41335. PMID: 27191498

30. Cruz, Gladys Mae Saquilabon, et al. "Femtosecond near-infrared laser microirradiation reveals a crucial role for PARP signaling on factor assemblies at DNA damage sites." Nucleic acids research (2015): gkv976. PMID: 26424850

物理外观	Solid
CAS号	763113-22-0
分子式	C₂₄H₂₃FN₄O₃
分子量	434.46
小分子别名	Olaparib
化学名称	4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one
溶解度	≥21.72 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
SMILES	O=C(C1CC1)N(CC1)CCN1C(c(cc(CC(c1c2cccc1)=NNC2=O)cc1)c1F)=O
存储条件	-20°C
运输条件	蓝冰
SDF文件	Download SDF

文件下载	文件内容	资源说明
	A4154-奥拉帕尼	操作手册
	A4154-奥拉帕尼相关单页	宣传单页

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奥拉帕尼

IC50和靶点

产品组分

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注意事项

FAQ