AG14361
Based on 7 publication(s) in Google Scholar
AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.42%
- CAS 番号: 328543-09-5
- 分子式: C19H20N4O
- 分子量:320.39
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Bioactive Compound Library Max
HY-L181
-
Epigenetics Compound Library Mini
HY-L005M
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
MedChemExpress（MCE）の使用を引用している文献 AG14361
More- Nat Methods. 2023 Sep;20(9):1388-1399. [Abstract]
- Breast Cancer Res. 2025 Oct 23;27(1):184. [Abstract]
- Eur J Pharmacol. 2024 Jun 19:176765. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Sci Rep. 2026 Mar 5;16(1):12110. [Abstract]
- EJNMMI Res. 2025 Apr 29;15(1):50. [Abstract]
- Patent. US20180263995A1.
生物活性
|
PARP-1 0.5 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| LoVo | GI50 |
11.2 μM
Compound: 22
|
Concentration that gives 50% growth inhibition in LoVo cells, activity expressed as GI50
Concentration that gives 50% growth inhibition in LoVo cells, activity expressed as GI50
|
[PMID: 12519059] |
AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively. AG14361 inhibits the proliferation of human cancer cells, such as A549, LoVo, and SW620 cells, with GI50s of 14 μM, 11.2 μM and 20 μM, respectively. Furthermore, AG14361 in combination with NSC 362856 markedly reduces the GI50 value of NSC 362856 in LoVo and A549 cells, but does not exert such an effect in SW620 cells[1]. AG14361 suppresses breast cancer cells with IC50s of 17 μM and 25 μM for 92 J-wt-BRCA1 and 92 J-sh-BRCA1 cells, respectively. AG14361 induces caspase 3/7 activation and cell cycle abnormalities, and also inhibits NF-κB signaling[2]. AG14361 (0.4 μM) enhances the growth-inhibitory and cytotoxic effects of topoisomerase I poisons, with no obvious effect on the formation and reversal of cleavable complexes, and increases the persistence of camptothecin-induced DNA single-strand breaks[3].
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.
化学情報
-
CAS 番号 328543-09-5
-
性状 Solid
-
分子量 320.39
-
分子式 C19H20N4O
-
Color White to off-white
-
SMILES
O=C1NCCN2C3=C1C=CC=C3N=C2C4=CC=C(C=C4)CN(C)C
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
Nat Methods
2023 Sep;20(9):1388-1399. PMID: 37474806 -
Breast Cancer Res
Modulating phosphodiesterase-5 activity to suppress the immunosuppressive mechanisms of myeloid-derived suppressor cells in breast cancer. [Abstract]2025 Oct 23;27(1):184. PMID: 41131545 -
Eur J Pharmacol
PARP-1 dependent cell death pathway (Parthanatos) mediates early brain injury after subarachnoid hemorrhage. [Abstract]2024 Jun 19:176765. PMID: 38906236 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Sci Rep
Propofol regulates METTL3-mediated PARP-1 m6A modification to promote Parthanatos to improve NSCLC chemotherapy resistance. [Abstract]2026 Mar 5;16(1):12110. PMID: 41781454 -
EJNMMI Res
Evaluation of a simplified radiolabeling method for a PARP inhibitor in an animal model of breast cancer. [Abstract]2025 Apr 29;15(1):50. PMID: 40301197 -
溶剤 & 溶解度
DMSO : 10 mg/mL (31.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 1 mg/mL (3.12 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (3.12 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
プロトコル
The activity of full-length recombinant human PARP-1 is measured in a reaction mixture containing 20 nM PARP-1, 500 μM NAD+ plus [32P]NAD+ (0.1-0.3 μCi per reaction mixture), and activated calf thymus DNA (10 μg/mL) at 25°C; the reaction is terminated after 4 minutes by adding ice-cold 10% (wt/vol) trichloroacetic acid. The reaction product [32P]ADP-ribose incorporated into acid-insoluble material is deposited onto Whatman GF/C glass fiber filters with a microfiltration apparatus and quantified with a PhosphorImager. Inhibition of PARP-1 activity by AG14361 at 0-600 nM is measured, and the Ki for AG14361 is calculated by nonlinear regression analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell viability assay is performed using a luciferase-coupled ATP quantization assay of metabolically active cells in a 96-well plate and MTT. For MTT, 1 to 2 × 104 cells are plated per one well of a 24-well plate. Target drugs (AG14361) at various concentrations are dissolved in DMSO and then added to the cells in 10% fetal bovine serum-containing Dulbecco’s modified Eagle’s medium (DMEM), IC50 concentration of AG14361 are also added to each well. The final DMSO concentration is kept at 0.1% after the addition to medium. After 48 hr medium is removed and 0.3 mL of 0.1% MTT in phosphate-buffered saline (PBS) is added in each well. After incubation for 30 min in a 37°C CO2 incubator, MTT solution is removed and 0.8 mL of 2-propanol is added. After shaking for 30 min, OD560 is measured using a plate reader. Plating for each time point is done in triplicate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CD-1 nude mice bearing palpable, subcutaneous SW620 or LoVo xenografts are treated intraperitoneally with normal saline (control animals) or AG14361 (at 5 or 15 mg/kg) alone daily for 5 days (five mice per group). For drug combinations, AG14361 is administered intraperitoneally daily for 5 days immediately before administering the cytotoxic drug (NSC 362856 at 68 mg/kg orally or CPT-11 at 2.5 mg/kg intraperitoneally) or 30 minutes before applying 2 Gy of x-irradiation locally to the tumor daily for 5 days. Tumor volumes, determined from two-dimensional caliper measurements and the equation a2 × b/2 (where a is the width and b is the length of the tumor), are presented as median relative tumor volume (RTV). That is, RTV1 is the tumor volume on the initial day of treatment (day 0), and RTV4 is the tumor volume 4 times that on the initial day of treatment. Tumor growth delay is defined as the time to RTV4 in drug-treated or irradiated mice compared with the time to RTV4 in control (vehicle alone) mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (283 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Calabrese CR, et al. Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361. J Natl Cancer Inst. 2004 Jan 7;96(1):56-67. [Content Brief]
[2]. Vazquez-Ortiz G, et al. Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells. Breast Cancer Res. 2014 Jun 24;16(3):R67. [Content Brief]
[3]. Smith LM, et al. The novel poly(ADP-Ribose) polymerase inhibitor, AG14361, sensitizes cells to topoisomerase I poisons by increasing the persistence of DNA strand breaks. Clin Cancer Res. 2005 Dec 1;11(23):8449-57. [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 | 3.1212 mL | 15.6060 mL | 31.2120 mL | 78.0299 mL |
| 5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL | 15.6060 mL | |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL | 7.8030 mL | |
| 15 mM | 0.2081 mL | 1.0404 mL | 2.0808 mL | 5.2020 mL | |
| 20 mM | 0.1561 mL | 0.7803 mL | 1.5606 mL | 3.9015 mL | |
| 25 mM | 0.1248 mL | 0.6242 mL | 1.2485 mL | 3.1212 mL | |
| 30 mM | 0.1040 mL | 0.5202 mL | 1.0404 mL | 2.6010 mL |
AG14361 関連分類
HY-12032 関連分類
Powered by Bioz