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| Other Sizes |
| Targets |
PARP1 and PARP2. 6(5H)-Phenanthridinone is an inhibitor of PARP1 and PARP2 with EC50 values of 10.2 and 36.3 μM, respectively, in yeast cells expressing the enzymes. PARP is involved in DNA repair and cellular response to DNA damage.
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| ln Vitro |
6(5H)-Phenanthridinone demonstrates inhibition of PARP1 and PARP2 in enzymatic assays. Treatment of cells with the compound and various DNA-damaging agents showed a resistance to apoptosis. It has immunosuppressive activity. Detailed IC50 values have been reported.
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| ln Vivo |
In vivo activity of 6(5H)-Phenanthridinone has not been extensively characterized. The compound is used as a research tool to study PARP function in cellular response to DNA damage. In vivo studies would be needed to evaluate its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays for PARP inhibition are performed using recombinant PARP1 or PARP2 enzymes in the presence of NAD+ and a DNA substrate. 6(5H)-Phenanthridinone is incubated at varying concentrations with the enzyme and substrate. PARP activity is measured by detection of ADP-ribose polymers. EC50 values are calculated from dose-response curves.
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| Cell Assay |
Cells are cultured and treated with 6(5H)-Phenanthridinone at concentrations typically ranging from 1–100 μM for 24–48 hours. PARP inhibition is assessed by measuring PARP activity or PAR levels by Western blot. Apoptosis is evaluated by caspase activation or Annexin V staining. Cell viability is assessed by standard assays.
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| Animal Protocol |
In vivo animal studies for 6(5H)-Phenanthridinone have not been reported in publicly available literature. The compound is primarily used as an in vitro research tool. Future studies in animal models of cancer or inflammation would be needed to evaluate in vivo efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 6(5H)-Phenanthridinone have not been published. The compound has a molecular weight of 195.22 and formula C13H9NO. Solubility information is limited. In vivo PK parameters such as half-life, bioavailability, and tissue distribution have not been characterized.
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| Toxicity/Toxicokinetics |
Toxicology data for 6(5H)-Phenanthridinone have not been published. The compound is for research use only and not approved for human therapeutic applications. No systematic toxicological evaluation has been performed. Standard safety precautions for handling chemical inhibitors should be observed.
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| References | |
| Additional Infomation |
Phenanthridone is a phenanthridine compound with an oxygen substituent introduced at the 6-position of phenanthridine. It is a poly(ADP-ribose) polymerase (PARP) inhibitor and has been shown to possess immunosuppressive activity. Phenanthridone exhibits dual action as a mutagen, immunosuppressant, and EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor. It is a lactam belonging to the phenanthridine class of compounds.
6(5H)-Phenanthridinone (CAS: 1015-89-0, molecular formula C13H9NO, molecular weight 195.22) is a PARP inhibitor. It has immunosuppressive activity. It is used as a research tool to study PARP function. It is not in clinical trials and has no regulatory approval. The compound is supplied as a research-grade inhibitor for laboratory use only. |
| Molecular Formula |
C13H9NO
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|---|---|
| Molecular Weight |
195.22
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| Exact Mass |
195.068
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| Elemental Analysis |
C, 79.98; H, 4.65; N, 7.17; O, 8.20
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| CAS # |
1015-89-0
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| PubChem CID |
1853
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
274.8±7.0 °C at 760 mmHg
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| Melting Point |
290-292 °C(lit.)
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| Flash Point |
158.7±3.1 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.642
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| LogP |
2.81
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
15
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| Complexity |
263
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C2=C([H])C([H])=C([H])C([H])=C2C2=C([H])C([H])=C([H])C([H])=C2N1[H]
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| InChi Key |
RZFVLEJOHSLEFR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H9NO/c15-13-11-7-2-1-5-9(11)10-6-3-4-8-12(10)14-13/h1-8H,(H,14,15)
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| Chemical Name |
5H-phenanthridin-6-one
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| Synonyms |
NSC 40943; NSC 11021; 6(5H)-Phenanthridinone; NSC 61083
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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 |
| 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 | 5.1224 mL | 25.6121 mL | 51.2243 mL | |
| 5 mM | 1.0245 mL | 5.1224 mL | 10.2449 mL | |
| 10 mM | 0.5122 mL | 2.5612 mL | 5.1224 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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