| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
5,15-Diphenylporphyrin targets STAT3 (signal transducer and activator of transcription 3), a transcription factor that plays a critical role in cell proliferation, survival, and immune regulation. STAT3 is frequently constitutively activated in many cancers, promoting tumor growth, metastasis, and immune evasion. By acting as a selective STAT3-SH2 antagonist, 5,15-diphenylporphyrin inhibits STAT3 dimerization and nuclear translocation, blocking STAT3-mediated transcriptional activity. Its selectivity for STAT3 over STAT1 (IC50 = 10 µM) supports its use as a specific probe for STAT3 function.
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| ln Vitro |
In vitro, 5,15-diphenylporphyrin is a selective STAT3-SH2 antagonist with an IC50 of 0.28 µM for STAT3 and 10 µM for STAT1. The compound inhibits STAT3 dimerization and DNA binding, blocking STAT3-mediated transcriptional activity. In cell-based assays, 5,15-diphenylporphyrin inhibits the proliferation of cancer cell lines with constitutively active STAT3 and induces apoptosis. Its activity is concentration-dependent, with effective concentrations in the nanomolar to micromolar range. Its selectivity for STAT3 over STAT1 makes it a valuable tool for studying STAT3 signaling and for developing novel anticancer therapeutics.
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| ln Vivo |
In vivo, 5,15-diphenylporphyrin has been studied in preclinical models of cancer. Its ability to inhibit STAT3 signaling may lead to antitumor effects in STAT3-dependent tumors. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying STAT3 signaling and cancer biology. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro STAT3-SH2 binding assay for 5,15-diphenylporphyrin typically uses purified STAT3 protein and a fluorescence polarization or ELISA-based assay to measure the inhibition of STAT3-SH2 domain binding to its phosphotyrosine peptide ligand. The compound is incubated with STAT3 protein and a fluorescently labeled or biotinylated peptide at varying concentrations (typically 0.1 nM to 10 µM). The inhibition of binding is measured, and IC50 values are calculated from dose-response curves using nonlinear regression. For STAT1 selectivity, the compound is tested against STAT1-SH2 in a similar assay. Positive controls and negative controls are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines with constitutively active STAT3 are treated with 5,15-diphenylporphyrin at concentrations ranging from 0.01 to 10 µM for 24-72 hours. Cell viability is assessed using CellTiter-Glo or MTT assays. STAT3 phosphorylation and nuclear translocation are assessed by Western blotting and immunofluorescence. STAT3 target gene expression (e.g., Bcl-2, Cyclin D1, Survivin) is assessed by qRT-PCR. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice are subcutaneously inoculated with cancer cells with constitutively active STAT3. When tumors reach a volume of approximately 100-200 mm³, mice are randomized into treatment groups (n=5-10 per group). 5,15-Diphenylporphyrin is administered orally or intraperitoneally at doses ranging from 1 to 50 mg/kg, typically once or twice daily, for 14-28 days. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity. At study endpoint, tumors are harvested for Western blot analysis of STAT3 phosphorylation and target gene expression, as well as for immunohistochemistry (Ki67, cleaved caspase-3). All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 5,15-diphenylporphyrin have been partially characterized. The compound has a molecular weight of 462.56 and a molecular formula of C32H22N4. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 4-8 hours. The compound distributes into tissues including tumor, liver, and kidney. Plasma protein binding is moderate to high. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of 5,15-diphenylporphyrin are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
5,15-Diphenylporphyrin is a selective STAT3-SH2 antagonist with IC50s of 0.28 µM for STAT3 and 10 µM for STAT1. It is used for studying STAT3 signaling and cancer biology. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥95%) for laboratory use only. Its selective STAT3 inhibition makes it a valuable tool for studying STAT3 signaling, cancer biology, and for developing novel anticancer therapeutics.
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| Molecular Formula |
C32H22N4
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| Molecular Weight |
462.5439
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| Exact Mass |
462.184
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| CAS # |
22112-89-6
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| PubChem CID |
10895852
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| Appearance |
Brown to black solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
912.3±65.0 °C at 760 mmHg
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| Flash Point |
401.3±27.2 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.705
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| LogP |
8.49
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
36
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| Complexity |
657
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QIBKIAFNCVIIMG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H22N4/c1-3-7-21(8-4-1)31-27-15-11-23(33-27)19-25-13-17-29(35-25)32(22-9-5-2-6-10-22)30-18-14-26(36-30)20-24-12-16-28(31)34-24/h1-20,33,35H
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| Chemical Name |
10,20-diphenyl-21,22-dihydroporphyrin
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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) |
DMSO : ~2 mg/mL (~4.32 mM)
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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 | 2.1620 mL | 10.8099 mL | 21.6198 mL | |
| 5 mM | 0.4324 mL | 2.1620 mL | 4.3240 mL | |
| 10 mM | 0.2162 mL | 1.0810 mL | 2.1620 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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