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| Targets |
Phenanthriplatin targets DNA through covalent binding, forming DNA adducts that disrupt DNA replication and transcription. It binds more effectively to 5'-deoxyguanosine monophosphate than to N-acetyl methionine, whereas pyriplatin reacts equally well with both reagents. The compound also acts as a covalent poison of topoisomerase II cleavage complexes. The hydrophobic phenanthridine ligand maximizes cellular uptake, rendering it more effective and cytotoxic compared with cisplatin and carboplatin.
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| ln Vitro |
Phenanthriplatin demonstrates significantly greater anticancer activity than cisplatin and oxaliplatin across various human cancer cell lines. In testicular cancer cells, IC50 values are 0.14 μM for phenanthriplatin vs 1.12 μM for cisplatin and 0.035 μM for oxaliplatin. In prostate cancer cells: 4.56 μM vs 13.2 μM (cisplatin) vs 0.74 μM (oxaliplatin). In lung cancer cells: 5.16 μM vs 47.9 μM (cisplatin). The compound also downregulates long non-coding RNAs involved in Wnt/β-catenin and TGF-β signaling pathways.
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| ln Vivo |
In vivo efficacy data for Phenanthriplatin are limited in the available literature. The compound is characterized as a potent anticancer agent with significantly greater activity than cisplatin and oxaliplatin, suggesting potential for enhanced in vivo efficacy. Its mechanism of DNA binding, crosslinking, and disruption of the DNA double helix leads to cell cycle arrest and apoptosis in rapidly dividing cancer cells. The hydrophobic phenanthridine ligand facilitates cellular uptake, which may translate to improved in vivo biodistribution and tumor penetration.
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| Enzyme Assay |
Cellular uptake of Phenanthriplatin is substantially greater than that of cisplatin and pyriplatin due to the hydrophobicity of the phenanthridine ligand. The compound is thought to penetrate cell membranes in its ionized form by either passive diffusion or carrier-mediated active transport. Binding assays to 5'-deoxyguanosine monophosphate versus N-acetyl methionine demonstrate preferential DNA binding. Enzyme assays with topoisomerase II show that phenanthriplatin acts as a covalent poison of topoisomerase II cleavage complexes.
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| Cell Assay |
In vitro cell-based cytotoxicity assays are performed using various human cancer cell lines including testicular (NTERA-2), prostate (PC3), and lung (A549) cancer cells. Cells are treated with phenanthriplatin at varying concentrations for 72 hours, and cell viability is assessed using standard assays such as MTT or SRB to determine IC50 values. The compound’s effects on long non-coding RNA expression and cancer signaling pathways are evaluated using qPCR and Western blot analysis.
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| Animal Protocol |
In vivo animal studies for Phenanthriplatin are not extensively detailed in the available literature. As a platinum-based anticancer agent, typical in vivo evaluation would involve xenograft mouse models bearing human tumor cell lines. Tumor-bearing mice would be treated with phenanthriplatin via intravenous administration, and tumor growth inhibition, survival rates, and body weight changes would be monitored. The compound’s superior in vitro cytotoxicity suggests potential for enhanced in vivo antitumor efficacy compared to cisplatin and oxaliplatin.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic properties of Phenanthriplatin are not extensively reported. The compound is a monovalent platinum(II) complex with a molecular weight of 503.80 g/mol. It is soluble in DMSO and appears as a solid powder. Cellular uptake is substantially greater than that of cisplatin and pyriplatin due to the hydrophobicity of the phenanthridine ligand. The compound penetrates cell membranes in its ionized form by either passive diffusion or carrier-mediated active transport. Stability: >2 years if stored properly at 0–4°C.
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| Toxicity/Toxicokinetics |
Toxicological data for Phenanthriplatin are limited in the available literature. As a platinum-based DNA-binding agent, expected toxicities would be similar to those of other platinum chemotherapeutics, including nephrotoxicity, neurotoxicity, and myelosuppression. The compound is classified for research use only and is not intended for human therapeutic use. Its significantly greater cytotoxicity compared to cisplatin and oxaliplatin suggests a potentially improved therapeutic index, though formal toxicological profiles are not detailed in the available sources.
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| References | |
| Additional Infomation |
Phenanthriplatin (CAS 1416900-51-0) is a research-stage platinum(II)-based anticancer agent with the IUPAC name cis-[Pt(NH3)2-(phenanthridine)Cl]NO3. It exhibits significantly greater activity than cisplatin and oxaliplatin and acts as a covalent poison of topoisomerase II cleavage complexes. The compound’s cellular uptake is substantially enhanced by the hydrophobic phenanthridine ligand. It has been studied for its effects on long non-coding RNAs in cancer signaling pathways. No clinical trial or approved indication data are available for this compound.
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| Molecular Formula |
C13H15CLN3PT.NO3
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| Molecular Weight |
505.82
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| Exact Mass |
503.0324
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| CAS # |
1416900-51-0
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| Appearance |
White to off-white solid powder
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| SMILES |
N([O-])(=O)=O.[Pt+2](N1C=C2C=CC=CC2=C2C=CC=CC=12)(N)(N)[Cl-]
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| Synonyms |
cis-[Pt(NH3)2-(phenanthridine)Cl]NO3; Phenanthriplatin
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 1.9770 mL | 9.8849 mL | 19.7699 mL | |
| 5 mM | 0.3954 mL | 1.9770 mL | 3.9540 mL | |
| 10 mM | 0.1977 mL | 0.9885 mL | 1.9770 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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