AZD-2461
Based on 10 publication(s) in Google Scholar
AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.
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- Purity: 99.79%
- CAS No.: 1174043-16-3
- 화학식: C22H22FN3O3
- 분자량:395.43
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AZD-2461
More- Clin Cancer Res. 2017 Feb 15;23(4):1001-1011. [Abstract]
- Neoplasia. 2025 May:63:101152. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Neurochem Res. 2026 Jun 12;51(3):192. [Abstract]
- Cell Biochem Funct. 2019 Oct;37(7):534-544. [Abstract]
- PLoS One. 2026 Apr 3;21(4):e0345514.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Patent. US20200129476A1
- Patent. US20200078369A1
- Patent. US20180362972A1.
Biological Activity
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PARP2 2 nM (IC50) |
PARP1 5 nM (IC50) |
PARP3 200 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
5 nM
Compound: 96g
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Inhibition of human HeLa cell derived PARP preincubated for 10 mins followed by NAD and double stranded DNA-oligos addition and measured after 45 mins by scintillation counting
Inhibition of human HeLa cell derived PARP preincubated for 10 mins followed by NAD and double stranded DNA-oligos addition and measured after 45 mins by scintillation counting
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[PMID: 31401008] |
| MCF-10A | IC50 |
>50 μM
Compound: Ola
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Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MCF7 | IC50 |
>50 μM
Compound: Ola
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Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MDA-MB-231 | IC50 |
36.92 μM
Compound: Ola
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MDA-MB-468 | IC50 |
35.57 μM
Compound: Ola
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Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 34455779] |
| MEF | EC50 |
14.9 μM
Compound: AZD2461
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Cytotoxicity against mouse PARP2 deficient MEF cells expressing PARP1 assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
Cytotoxicity against mouse PARP2 deficient MEF cells expressing PARP1 assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
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[PMID: 29856625] |
| MEF | EC50 |
22.1 μM
Compound: AZD2461
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Cytotoxicity against mouse wild type MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
Cytotoxicity against mouse wild type MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
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[PMID: 29856625] |
| MEF | EC50 |
49 μM
Compound: AZD2461
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Cytotoxicity against mouse PARP1 deficient MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
Cytotoxicity against mouse PARP1 deficient MEF cells assessed as reduction in cell viability after 4 to 7 days by cell-titer glo assay
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[PMID: 29856625] |
AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively. AZD-2461 (500 nM) shows inhibitory activity against DNA single-strand break repair in human A459 cells. AZD-2461 cuases resistance and high P-gp expression levels in BRCA2-deficient mouse breast cancer line KB2P3.4[1]. AZD-2461 is cytotoxic to BT-20 cells (5-50 μM), increases the proportions of S- and G2-phase BT-20 cells (5-20 μM), and weakly affects the progression of cell cycle in SKBr-3 cells (5-20 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1174043-16-3
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Appearance Solid
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분자량 395.43
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화학식 C22H22FN3O3
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Color White to off-white
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SMILES
O=C1NN=C(CC2=CC=C(F)C(C(N3CCC(OC)CC3)=O)=C2)C4=C1C=CC=C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Clin Cancer Res
Drug-Driven Synthetic Lethality: Bypassing Tumor Cell Genetics with a Combination of AsiDNA and PARP Inhibitors. [Abstract]2017 Feb 15;23(4):1001-1011. PMID: 27559053 -
Neoplasia
Targeting BARD1 suppresses a Myc-dependent transcriptional program and tumor growth in pancreatic ductal adenocarcinoma. [Abstract]2025 May:63:101152. PMID: 40096771 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Neurochem Res
β-Lapachone-Induced Oxidative Stress Causes PARP-Dependent NAD+-Depletion that Affects the Energy Metabolism of Cultured Primary Rat Astrocytes. [Abstract]2026 Jun 12;51(3):192. PMID: 42277481 -
Cell Biochem Funct
The CTIP-mediated repair of TNF-α-induced DNA double-strand break was impaired by miR-130b in cervical cancer cell. [Abstract]2019 Oct;37(7):534-544. PMID: 31418900 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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용액&용해도
DMSO : ≥ 100 mg/mL (252.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
BT-20 and SKBr-3 human primary breast cancer cell lines are used in the assay. SKBr-3 cells are cultivated in DMEM medium with 10% FCS and BT-20 in RPMI medium under an atmosphere containing 5% CO2. Twenty four hours after plating (at 60-70% confluence), the cells are treated with the PARP-1 inhibitors NU1025, AZD-2461, iniparib, olaparib, and rucaparib at concentrations ranging from 50 to 200 μM, 5 to 50 μM, 5 to 50 μM, 1 to 10 μM, and 0.3 to 10 μM, respectively, for durations indicated in figures 1-7[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Starting from 2 weeks after transplantation into mice, tumor size is monitored at least 3 times a week. All treatments are started when tumors reach a size of approximately 200 mm3. Olaparib (50 mg/kg intraperitoneally) and AZD-2461 (100 mg/kg per os) are given for 28 consecutive days, unless otherwise indicated. If tumors do not shrink below 50% of the initial volume, treatment is continued for another 28 days; otherwise, a new treatment cycle of 28 days is started when the relapsing tumor reaches a size of 100% of the original volume. AZD-2461 is diluted in 0.5% w/v hydroxypropyl methylcellulose in deionized water to a concentration of 10 mg/mL[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Oplustil O'Connor L, et al. The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models. Cancer Res. 2016 Oct 15;76(20):6084-6094. Epub 2016 Aug 22. [Content Brief]
[2]. Węsierska-Gądek J, et al. Differential Potential of Pharmacological PARP Inhibitors for Inhibiting Cell Proliferation and Inducing Apoptosis in Human Breast Cancer Cells. J Cell Biochem. 2015 Dec;116(12):2824-39. [Content Brief]
[3]. Jaspers JE, et al. Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov. 2013 Jan;3(1):68-81. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5289 mL | 12.6445 mL | 25.2889 mL | 63.2223 mL |
| 5 mM | 0.5058 mL | 2.5289 mL | 5.0578 mL | 12.6445 mL | |
| 10 mM | 0.2529 mL | 1.2644 mL | 2.5289 mL | 6.3222 mL | |
| 15 mM | 0.1686 mL | 0.8430 mL | 1.6859 mL | 4.2148 mL | |
| 20 mM | 0.1264 mL | 0.6322 mL | 1.2644 mL | 3.1611 mL | |
| 25 mM | 0.1012 mL | 0.5058 mL | 1.0116 mL | 2.5289 mL | |
| 30 mM | 0.0843 mL | 0.4215 mL | 0.8430 mL | 2.1074 mL | |
| 40 mM | 0.0632 mL | 0.3161 mL | 0.6322 mL | 1.5806 mL | |
| 50 mM | 0.0506 mL | 0.2529 mL | 0.5058 mL | 1.2644 mL | |
| 60 mM | 0.0421 mL | 0.2107 mL | 0.4215 mL | 1.0537 mL | |
| 80 mM | 0.0316 mL | 0.1581 mL | 0.3161 mL | 0.7903 mL | |
| 100 mM | 0.0253 mL | 0.1264 mL | 0.2529 mL | 0.6322 mL |
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