CAS Number763113-22-0
Synonyms1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine; AZD-2281; azd2281 Olaparib; 4-(3-{[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl}-4-fluorobenzyl)-1(2H)-phthalazinone; Olaparib; 4-(3-{[4-(Cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorobenzyl)phthalazin-1(2H)-one; Lynparza; AZD2281
Molecular FormulaC24H23FN4O3
Molecular Weight434.46
Purity≥98 (HPLC)%
Density1.4±0.1 g/cm3
Appearancepowder
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 763113-22-0 |
| Catalog No. | 2A-9058118 |
| Chinese Name | 奥拉帕尼 |
| Synonyms | 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine; AZD-2281; azd2281 Olaparib; 4-(3-{[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl}-4-fluorobenzyl)-1(2H)-phthalazinone; Olaparib; 4-(3-{[4-(Cyclopropylcarbonyl)piperazin-1-yl]carbonyl}-4-fluorobenzyl)phthalazin-1(2H)-one; Lynparza; AZD2281 |
| Molecular Formula | C24H23FN4O3 |
| Molecular Weight | 434.46 |
| Purity | ≥98 (HPLC) |
| Density | 1.4±0.1 g/cm3 |
| Appearance | powder |
| Storage Condition | 2~8℃ |
| Application | Olaparib (AZD2281; KU0059436) is a potent PARP inhibitor with IC50s of 5 and 1 nM for PARP-1 and PARP-2, respectively. |
| HTC | 2933990090 |
| MDL Number | MFCD13185161 |
| SMILES | Fc1c(cc(cc1)C=C4NNC(=O)c5c4cccc5)C(=O)N2CCN(CC2)C(=O)C3CC3 |
| 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/h1-5,8,13-14,16,26H,6-7,9-12H2,(H,27,30) |
| InChI Key | JQYIJKFTPJWNFM-UHFFFAOYSA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| MSDS | msds/58118_1_763113_22_0.pdf |
| Use of | Olaparib (AZD2281;KU0059436) is a potent and oral PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Properties Name olaparib Synonym More Synonyms Olaparib (AZD2281) Biological Activity Description Olaparib (AZD2281;KU0059436) is a potent and oral PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Related Catalog Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Autophagy >> Mitophagy Signaling Pathways >> Cell Cycle/DNA Damage >> PARP Signaling Pathways >> Epigenetics >> PARP Research Areas >> Cancer PARP-2:1 nM (IC50) PARP-1:5 nM (IC50) tankyrase-1:1.5 μM (IC50) Kinase Assay 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]. References [1]. 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 [2]. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58. [3]. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 and Cisplatin in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272. [4]. Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351. Chemical & Physical Properties Molecular Formula C24H23FN4O3 Exact Mass 434.175415 PSA 86.37000 Index of Refraction 1.702 InChIKey FDLYAMZZIXQODN-UHFFFAOYSA-N Storage condition 2~8℃ Safety Information Hazard Codes Xi Risk Phrases 22-38-37-36 HS Code 2933990090 |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
| Related Products in API & Advanced Intermediates | ||
|---|---|---|
| Sitagliptin phosphate monohydrate | 654671-77-9 | 2A-9057813 |
| Sitagliptin phosphate | 654671-78-0 | 2A-9057814 |
| Linagliptin | 668270-12-0 | 2A-0202309 |
| Neratinib | 698387-09-6 | 2A-9057939 |
| Regorafenib | 755037-03-7 | 2A-9058087 |
| Canagliflozin | 842133-18-0 | 2A-9058288 |
| Alogliptin benzoate | 850649-62-6 | 2A-9058379 |
| Rosuvastatin ethyl ester | 851443-04-4 | 2A-9058399 |
| Raltegravir potassium | 871038-72-1 | 2A-9058636 |
| Vismodegib | 879085-55-9 | 2A-9058733 |
| Browse all API & Advanced Intermediates products » | ||
Phone:
630-322-8886
630-322-8887
Email:
Office Locations:
Chicago, IL, USA
San Francisco, CA, USA
EN
SDS