Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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O126162-10mg | 10mg | In stock | $45.90 | |
O126162-25mg | 25mg | In stock | $59.90 | |
O126162-100mg | 100mg | In stock | $79.90 | |
O126162-250mg | 250mg | In stock | $95.90 | |
O126162-1g | 1g | In stock | $235.90 | |
O126162-5g | 5g | In stock | $915.90 |
Synonyms | KU-0059436 | KU0059436 | KU-0059436 | 4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one | 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one | Lynparza | DTXSID6 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Olaparib is a potent inhibitor of both PARP-1 and PARP-2, with IC50 = 5 nM and 1 nM, respectively. Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-str |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | PARP 1, 2 and 3 inhibitor |
Note | 10mg卖完停产,不再备货 |
Product Description | Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM, 300-times less effective against tankyrase-1. |
ALogP | 1.9 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-[[3-[4-(cyclopropanecarbonyl)piperazine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one |
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INCHI | InChI=1S/C24H23FN4O3/c25-20-8-5-15(14-21-17-3-1-2-4-18(17)22(30)27-26-21)13-19(20)24(32)29-11-9-28(10-12-29)23(31)16-6-7-16/h1-5,8,13,16H,6-7,9-12,14H2,(H,27,30) |
InChi Key | FDLYAMZZIXQODN-UHFFFAOYSA-N |
Canonical SMILES | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F |
Isomeric SMILES | C1CC1C(=O)N2CCN(CC2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F |
Alternate CAS | 763113-22-0 |
PubChem CID | 23725625 |
NSC Number | 747856 |
MeSH Entry Terms | AZD 2281;AZD-2281;AZD221;AZD2281;Lynparza;olaparib |
Molecular Weight | 434.46 |
ChEMBL Ligand | CHEMBL521686 |
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PubChem CID | 23725625 |
CAS Registry No. | 763113-22-0 |
Wikipedia | Olaparib |
RCSB PDB Ligand | 09L |
DrugCentral Ligand | 4907 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
A2306817 | Certificate of Analysis | Oct 15, 2024 | O126162 |
A2306815 | Certificate of Analysis | Oct 15, 2024 | O126162 |
A2306809 | Certificate of Analysis | Oct 15, 2024 | O126162 |
A2306807 | Certificate of Analysis | Oct 15, 2024 | O126162 |
A2306805 | Certificate of Analysis | Oct 15, 2024 | O126162 |
A2306804 | Certificate of Analysis | Oct 10, 2024 | O126162 |
A2306806 | Certificate of Analysis | Oct 10, 2024 | O126162 |
A2306808 | Certificate of Analysis | Oct 10, 2024 | O126162 |
A2306813 | Certificate of Analysis | Oct 10, 2024 | O126162 |
A2306816 | Certificate of Analysis | Oct 10, 2024 | O126162 |
A2211819 | Certificate of Analysis | Oct 13, 2023 | O126162 |
D1810189 | Certificate of Analysis | Oct 13, 2023 | O126162 |
H2305139 | Certificate of Analysis | Jul 20, 2023 | O126162 |
H2305136 | Certificate of Analysis | Jul 20, 2023 | O126162 |
H2305124 | Certificate of Analysis | Jul 20, 2023 | O126162 |
E2411012 | Certificate of Analysis | Jul 20, 2023 | O126162 |
B2428145 | Certificate of Analysis | Jul 20, 2023 | O126162 |
I2128322 | Certificate of Analysis | Jul 10, 2023 | O126162 |
G1521076 | Certificate of Analysis | Feb 03, 2023 | O126162 |
I2223351 | Certificate of Analysis | Sep 27, 2022 | O126162 |
I2223358 | Certificate of Analysis | Sep 27, 2022 | O126162 |
A2211471 | Certificate of Analysis | Dec 22, 2021 | O126162 |
A2211467 | Certificate of Analysis | Dec 22, 2021 | O126162 |
A2211457 | Certificate of Analysis | Dec 22, 2021 | O126162 |
Solubility | Soluble in DMSO (33 mg/mL), ethanol (1.7 mg/mL), and water (<1 mg/mL) at 25 °C. |
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Pictogram(s) | GHS06, GHS08, GHS07 |
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Signal | Danger |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H301:Toxic if swallowed H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H361:Suspected of damaging fertility or the unborn child |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
1. Weimin Fang, Jinghao Wang, Xiaocong Ma, Ni Shao, Kunlin Ye, Dong Zhang, Changzheng Shi, Liangping Luo. (2023) A Progressively Disassembled DNA Repair Inhibitors Nanosystem for the Treatment of BRCA Wild-Type Triple-Negative Breast Cancer. International Journal of Nanomedicine, [PMID:37901361] |
2. Teng Wang, Jiaojiao Tao, Bingjie Wang, Tianze Jiang, Xia Zhao, Yang Yu, Xin Meng. (2023) Reversing Resistance of Cancer Stem Cells and Enhancing Pdt Based on Hyaluronic Acid Nanomicelles for Preventing Cancer Recurrence and Metastasis. Advanced Healthcare Materials, (9): (2302597). [PMID:37941492] |
3. Teng Wang, Yang Yu, Bingjie Wang, Tianze Jiang, Xin Meng, Xia Zhao. (2023) Photothermal hyaluronic acid composite hydrogel targeting cancer stem cells for inhibiting recurrence and metastasis of breast cancer. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 252 (126358). [PMID:37598824] |
4. Yang Yu, Teng Wang, Xin Meng, Tianze Jiang, Xia Zhao. (2023) Chitosan Thermosensitive Hydrogel Based on DNA Damage Repair Inhibition and Mild Photothermal Therapy for Enhanced Antitumor Treatment. BIOMACROMOLECULES, [PMID:37506051] |
5. Huiling Zhou, Chenxin Duan, Huimin Qin, Chaonan Huang, Jingxuan Hou, Yanming Chen, Jin Zhu, Cangcang Xu, Jian Jin, Tao Zhuang. (2023) Synthesis and structural characterization of a novel palbociclib-kaempferol cocrystal with improved tabletability and synergistic antitumor activity. JOURNAL OF MOLECULAR STRUCTURE, 1281 (135101). [PMID:] |
6. Ren-Jiang Kong, Xin-Yu Li, Jia-Qi Huang, Xiang Zhou, Fu-An Deng, Yan-Mei Li, Ling-Shan Liu, Shi-Ying Li, Hong Cheng. (2022) A self-delivery photodynamic sensitizer for enhanced DNA damage by PARP inhibition. Biomaterials Science, 11 (1): (162-169). [PMID:36398488] |
7. Chenxin Duan, Yanming Chen, Yuxin Zhang, Feifei Liang, Wenwen Liu, Xinyi Xiao, Cangcang Xu, Tao Zhuang, Chao Hao, Yin Chen. (2022) Two Cocrystals of Olaparib with Flavonoids toward Sustained Release: Structure, Dissolution Behavior, and Anticancer Activity Analysis. CRYSTAL GROWTH & DESIGN, 22 (8): (4885–4894). [PMID:] |
8. Huiping Hu, Yu Zhang, Wenting Ji, Hao Mei, Tingting Wu, Zihao He, Kaiping Wang, Chen Shi. (2022) Hyaluronic acid-coated and Olaparib-loaded PEI − PLGA nanoparticles for the targeted therapy of triple negative breast cancer. JOURNAL OF MICROENCAPSULATION, 39 (1): (25-36). [PMID:34859741] |
9. Jiejie Sun, Jingzhou Liu, Chunhong Gao, Jinpeng Zheng, Jinbang Zhang, Yaning Ding, Wei Gong, Meiyan Yang, Zhiping Li, Yuli Wang, Yang Yang, Chunsheng Gao. (2022) Targeted delivery of PARP inhibitors to neuronal mitochondria via biomimetic engineered nanosystems in a mouse model of traumatic brain injury. Acta Biomaterialia, 140 (573). [PMID:34958970] |
10. Meng Ding, Lei Xu, Yumeng Zhang, Wei Li, Yuqing Zhao. (2021) Simultaneous quantification and ADME prediction of AD-1 and its eight metabolites in rat feces, and screening of PARP-1 inhibitors through molecular docking. JOURNAL OF MOLECULAR STRUCTURE, 1244 (131016). [PMID:] |
1. Menear KA, Adcock C, Boulter R, Cockcroft XL, Copsey L, Cranston A, Dillon KJ, Drzewiecki J, Garman S, Gomez S et al.. (2008) 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, 51 (20): (6581-91). [PMID:18800822] |
2. Rottenberg S, Jaspers JE, Kersbergen A, van der Burg E, Nygren AO, Zander SA, Derksen PW, de Bruin M, Zevenhoven J, Lau A et al.. (2008) High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs.. Proc Natl Acad Sci USA, 105 (44): (17079-84). [PMID:18971340] |
3. Mateo J, Carreira S, Sandhu S, Miranda S, Mossop H, Perez-Lopez R, Nava Rodrigues D, Robinson D, Omlin A, Tunariu N et al.. (2015) DNA-Repair Defects and Olaparib in Metastatic Prostate Cancer.. N Engl J Med, 373 (18): (1697-708). [PMID:26510020] |
4. Clarke N, Wiechno P, Alekseev B, Sala N, Jones R, Kocak I, Chiuri VE, Jassem J, Fléchon A, Redfern C et al.. (2018) Olaparib combined with abiraterone in patients with metastatic castration-resistant prostate cancer: a randomised, double-blind, placebo-controlled, phase 2 trial.. Lancet Oncol, 19 (7): (975-986). [PMID:29880291] |
5. Ma Y, He L, Huang Q, Zheng S, Zhang Z, Li H, Liu S. (2018) Response to olaparib in metastatic castration-resistant prostate cancer with germline BRCA2 mutation: a case report.. BMC Med Genet, 19 (1): (185). [PMID:30333000] |
6. Karzai F, VanderWeele D, Madan RA, Owens H, Cordes LM, Hankin A, Couvillon A, Nichols E, Bilusic M, Beshiri ML et al.. (2018) Activity of durvalumab plus olaparib in metastatic castration-resistant prostate cancer in men with and without DNA damage repair mutations.. J Immunother Cancer, 6 (1): (141). [PMID:30514390] |
7. Buisson R, Dion-Côté AM, Coulombe Y, Launay H, Cai H, Stasiak AZ, Stasiak A, Xia B, Masson JY. (2010) Cooperation of breast cancer proteins PALB2 and piccolo BRCA2 in stimulating homologous recombination.. Nat Struct Mol Biol, 17 (10): (1247-54). [PMID:20871615] |
8. Murai J, Huang SY, Das BB, Renaud A, Zhang Y, Doroshow JH, Ji J, Takeda S, Pommier Y. (2012) Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors.. Cancer Res, 72 (21): (5588-99). [PMID:23118055] |
9. Cook D, Brown D, Alexander R, March R, Morgan P, Satterthwaite G, Pangalos MN. (2014) Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework.. Nat Rev Drug Discov, 13 (6): (419-31). [PMID:24833294] |
10. Weimin Fang, Jinghao Wang, Xiaocong Ma, Ni Shao, Kunlin Ye, Dong Zhang, Changzheng Shi, Liangping Luo. (2023) A Progressively Disassembled DNA Repair Inhibitors Nanosystem for the Treatment of BRCA Wild-Type Triple-Negative Breast Cancer. International Journal of Nanomedicine, [PMID:37901361] |
11. Teng Wang, Jiaojiao Tao, Bingjie Wang, Tianze Jiang, Xia Zhao, Yang Yu, Xin Meng. (2023) Reversing Resistance of Cancer Stem Cells and Enhancing Pdt Based on Hyaluronic Acid Nanomicelles for Preventing Cancer Recurrence and Metastasis. Advanced Healthcare Materials, (9): (2302597). [PMID:37941492] |
12. Teng Wang, Yang Yu, Bingjie Wang, Tianze Jiang, Xin Meng, Xia Zhao. (2023) Photothermal hyaluronic acid composite hydrogel targeting cancer stem cells for inhibiting recurrence and metastasis of breast cancer. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, 252 (126358). [PMID:37598824] |
13. Yang Yu, Teng Wang, Xin Meng, Tianze Jiang, Xia Zhao. (2023) Chitosan Thermosensitive Hydrogel Based on DNA Damage Repair Inhibition and Mild Photothermal Therapy for Enhanced Antitumor Treatment. BIOMACROMOLECULES, [PMID:37506051] |
14. Huiling Zhou, Chenxin Duan, Huimin Qin, Chaonan Huang, Jingxuan Hou, Yanming Chen, Jin Zhu, Cangcang Xu, Jian Jin, Tao Zhuang. (2023) Synthesis and structural characterization of a novel palbociclib-kaempferol cocrystal with improved tabletability and synergistic antitumor activity. JOURNAL OF MOLECULAR STRUCTURE, 1281 (135101). [PMID:] |
15. Ren-Jiang Kong, Xin-Yu Li, Jia-Qi Huang, Xiang Zhou, Fu-An Deng, Yan-Mei Li, Ling-Shan Liu, Shi-Ying Li, Hong Cheng. (2022) A self-delivery photodynamic sensitizer for enhanced DNA damage by PARP inhibition. Biomaterials Science, 11 (1): (162-169). [PMID:36398488] |
16. Chenxin Duan, Yanming Chen, Yuxin Zhang, Feifei Liang, Wenwen Liu, Xinyi Xiao, Cangcang Xu, Tao Zhuang, Chao Hao, Yin Chen. (2022) Two Cocrystals of Olaparib with Flavonoids toward Sustained Release: Structure, Dissolution Behavior, and Anticancer Activity Analysis. CRYSTAL GROWTH & DESIGN, 22 (8): (4885–4894). [PMID:] |
17. Huiping Hu, Yu Zhang, Wenting Ji, Hao Mei, Tingting Wu, Zihao He, Kaiping Wang, Chen Shi. (2022) Hyaluronic acid-coated and Olaparib-loaded PEI − PLGA nanoparticles for the targeted therapy of triple negative breast cancer. JOURNAL OF MICROENCAPSULATION, 39 (1): (25-36). [PMID:34859741] |
18. Jiejie Sun, Jingzhou Liu, Chunhong Gao, Jinpeng Zheng, Jinbang Zhang, Yaning Ding, Wei Gong, Meiyan Yang, Zhiping Li, Yuli Wang, Yang Yang, Chunsheng Gao. (2022) Targeted delivery of PARP inhibitors to neuronal mitochondria via biomimetic engineered nanosystems in a mouse model of traumatic brain injury. Acta Biomaterialia, 140 (573). [PMID:34958970] |
19. Meng Ding, Lei Xu, Yumeng Zhang, Wei Li, Yuqing Zhao. (2021) Simultaneous quantification and ADME prediction of AD-1 and its eight metabolites in rat feces, and screening of PARP-1 inhibitors through molecular docking. JOURNAL OF MOLECULAR STRUCTURE, 1244 (131016). [PMID:] |