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Purity: ≥98%
AG14361 (AG-14361) is a novel, potent and selective inhibitor of poly (ADP-ribose) polymerase-1 (PARP1) with potential anticancer activity. In a cell-free assay, it inhibits PARP1 with a Ki of less than 5 nM. It also exhibits strong in vivo antitumor efficacy and strong antiproliferative activity against a variety of cancer cells.
| Targets |
PARP-1 ( Ki = 0.5 nM )
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| ln Vitro |
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| Enzyme Assay |
Full-length recombinant human PARP-1 activity is assessed in a reaction mixture containing activated calf thymus DNA (10 μg/mL) at 25 °C, 500 μM NAD+ plus [32P]NAD+ (0.1–0.3 μCi per reaction mixture), and 20 nM PARP-1. The reaction is stopped after 4 minutes by adding ice-cold 10% (wt/vol) trichloroacetic acid. A PhosphorImager is used to quantify the reaction product [32P]ADP-ribose that is integrated into acid-insoluble material after it has been deposited onto Whatman GF/C glass fiber filters using a Bio-Dot microfiltration device. Inhibition of PARP-1 activity by AG14361 at 0–600 nM is measured, and the Ki for AG14361 is calculated by nonlinear regression analysis.
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| Cell Assay |
The luciferase-coupled ATP quantization assay of metabolically active cells in a 96-well plate is used in the cell viability assay along with MTT. One well of a 24-well plate is plated with one to two × 104 cells for MTT. The target medications (AG14361) are dissolved in DMSO at different concentrations and subsequently added to the cells in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal bovine serum. Additionally, each well receives an addition of the IC50 concentration of AG14361. The addition to medium results in a final DMSO concentration of 0.1%. The medium is removed after 48 hours, and each well receives 0.3 mL of 0.1% MTT in phosphate-buffered saline (PBS). The MTT solution is removed and 0.8 mL of 2-propanol is added after 30 minutes of incubation in a 37°C CO2 incubator. A plate reader is used to measure the OD560 following 30 minutes of shaking. Every time point is platented three times.
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| Animal Protocol |
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| References |
| Molecular Formula |
C19H20N4O
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| Molecular Weight |
320.39
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| Exact Mass |
320.16
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| Elemental Analysis |
C, 71.23; H, 6.29; N, 17.49; O, 4.99
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| CAS # |
328543-09-5
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CN(C)CC1=CC=C(C=C1)C2=NC3=CC=CC4=C3N2CCNC4=O
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| InChi Key |
SEKJSSBJKFLZIT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20N4O/c1-22(2)12-13-6-8-14(9-7-13)18-21-16-5-3-4-15-17(16)23(18)11-10-20-19(15)24/h3-9H,10-12H2,1-2H3,(H,20,24)
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| Chemical Name |
2-[4-[(dimethylamino)methyl]phenyl]-1,3,10-triazatricyclo[6.4.1.04,13]trideca-2,4,6,8(13)-tetraen-9-one
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| Synonyms |
AG 14361; AG14361; AG-14361
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (3.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 4% DMSO+ddH2O: 2mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1212 mL | 15.6060 mL | 31.2120 mL | |
| 5 mM | 0.6242 mL | 3.1212 mL | 6.2424 mL | |
| 10 mM | 0.3121 mL | 1.5606 mL | 3.1212 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effect of AG14361 on topo I poison-induced growth inhibition and cytotoxicity in PARP-1+/+, PARP-1−/−, and human leukemia cell lines.Clin Cancer Res. 2005 Dec 1;11(23):8449-57. |
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Effect of AG14361 on camptothecin-stabilized cleavable complex induction and removal.Clin Cancer Res. 2005 Dec 1;11(23):8449-57. |
Repair of camptothecin-induced DNA single-strand breaks in K562 cells in the presence or absence of AG14361.K562 cells were exposed to 30 nmol/L camptothecin for 30 minutes followed by repair in drug-free medium (white columns) or medium containing 0.4 μmol/L AG14361 (black columns) for 0, 10, or 20 minutes. DNA strand breaks were measured by alkaline elution. Relative elution was calculated by comparison with DMSO or 0.4 μmol/L AG14361 alone control as appropriate. Columns, mean of three independent experiments; bars, SE.Clin Cancer Res. 2005 Dec 1;11(23):8449-57. |
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