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| Targets |
4-Aminonaphthalimide targets PARP (poly(ADP-ribose) polymerase), an enzyme that plays a critical role in DNA repair by catalyzing the addition of ADP-ribose units to target proteins. The compound is a potent PARP inhibitor with an IC₅₀ of 180 nM. By inhibiting PARP, 4-Aminonaphthalimide blocks radiation-induced PARP activation in cancer cells, thereby potentiating the cytotoxicity of gamma radiation.
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| ln Vitro |
In vitro, 4-Aminonaphthalimide has been shown to be a potent PARP inhibitor with an IC₅₀ of 180 nM. The compound potentiates the cytotoxicity of gamma radiation in cancer cells but is not cytotoxic in the absence of radiation. It is used to study the role of PARP activity in various cell systems and sensitizes cancer/tumor cells to radiation-induced cell toxicity.
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| ln Vivo |
In vivo, 4-Aminonaphthalimide has been studied for its effects on PARP inhibition and radiation sensitization in animal models of cancer. The compound is typically administered to study its potential as a radiosensitizer in cancer therapy. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature.
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| Enzyme Assay |
4-Aminonaphthalimide's PARP inhibition activity has been characterized in enzyme assays. The compound has an IC₅₀ of 180 nM for PARP inhibition. Binding assays typically involve measuring the inhibition of PARP-mediated poly(ADP-ribose) synthesis using purified PARP enzyme or cell lysates. The compound is used to study the role of PARP in DNA repair and cell survival.
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| Cell Assay |
In vitro cell experiments with 4-Aminonaphthalimide typically use cancer cell lines to study PARP inhibition and radiation sensitization. Cells are treated with the compound at various concentrations, with or without gamma radiation exposure. Cell viability is assessed using standard cytotoxicity assays, and PARP activity is measured using biochemical assays. The compound's effects on DNA repair and cell death are also evaluated.
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| Animal Protocol |
In vivo animal studies with 4-Aminonaphthalimide have been conducted using rodent models of cancer to study radiation sensitization. The compound is typically administered prior to or concurrent with radiation therapy. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data specific to 4-Aminonaphthalimide are limited in the available literature. As a small molecule PARP inhibitor, the compound is expected to have reasonable bioavailability and tissue penetration. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
Toxicological data for 4-Aminonaphthalimide are limited. The compound is not cytotoxic in the absence of radiation, suggesting a favorable safety profile when used as a radiosensitizer. However, comprehensive toxicological studies have not been extensively reported. As a research compound, it is intended for laboratory use only and not for human consumption.
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| References | |
| Additional Infomation |
4-Amino-1,8-naphthylimide is a benzoisoquinoline and dicarboxylate.
4-Aminonaphthalimide (4-Amino-1,8-naphthalimide, 4-ANI) is a potent PARP inhibitor with an IC₅₀ of 180 nM. It has a molecular formula of C₁₂H₈N₂O₂ and a molecular weight of 212.20. The compound sensitizes cancer cells to gamma radiation-induced cytotoxicity and is used to study the role of PARP activity in various cell systems. It is available with a purity of 95%. |
| Molecular Formula |
C12H8N2O2
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|---|---|
| Molecular Weight |
212.20412
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| Exact Mass |
212.059
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| CAS # |
1742-95-6
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| PubChem CID |
1720
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| Appearance |
Yellow to brown solid powder
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| Density |
1.105 g/mL at 25ºC(lit.)
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| Boiling Point |
544.1ºC at 760 mmHg
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| Melting Point |
360ºC
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| Flash Point |
282.8ºC
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| Vapour Pressure |
6.75E-12mmHg at 25°C
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| Index of Refraction |
1.764
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| LogP |
1.642
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
16
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| Complexity |
342
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SSMIFVHARFVINF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H8N2O2/c13-9-5-4-8-10-6(9)2-1-3-7(10)11(15)14-12(8)16/h1-5H,13H2,(H,14,15,16)
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| Chemical Name |
6-aminobenzo[de]isoquinoline-1,3-dione
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7125 mL | 23.5627 mL | 47.1254 mL | |
| 5 mM | 0.9425 mL | 4.7125 mL | 9.4251 mL | |
| 10 mM | 0.4713 mL | 2.3563 mL | 4.7125 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.
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