| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
H2TMpyP-2 targets multiple molecular structures: (1) It intercalates into G-quadruplex DNA structures, binding with high affinity and stabilizing them, thereby inhibiting telomerase extension activity. (2) Upon light activation, it generates reactive singlet oxygen species (¹O2) that cause oxidative damage to cellular components, leading to cell death.
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|---|---|
| ln Vitro |
In cell-free assays, H2TMpyP-2 exhibits high singlet oxygen quantum yield (Φdelta ~0.5-0.7). It binds to G-quadruplex DNA with dissociation constants in the nanomolar to low micromolar range (Kd ~0.1-5 uM). The absorption spectrum shows a Soret band at approximately 422 nm and Q-bands between 500-650 nm, with a molar extinction coefficient of >200,000 M-¹cm-¹ at the Soret maximum.
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| ln Vivo |
In vivo, H2TMpyP-2 has been studied in animal models of cancer as a photosensitizer for PDT. When administered intravenously and activated with light at the tumor site, it generates cytotoxic singlet oxygen, leading to tumor cell death, vascular shutdown, and immune activation. It also shows efficacy in models of infectious diseases and macular degeneration.
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| Enzyme Assay |
For G-quadruplex binding assays, H2TMpyP-2 (0.5-10 uM) is incubated with G-quadruplex DNA (e.g., telomeric or c-Myc sequence) in a buffer (10 mM Tris-HCl, pH 7.4, 100 mM KCl) at 25degC. Binding affinity is measured by fluorescence spectroscopy (Ex/Em: 420/650 nm) or circular dichroism to monitor the induced conformational changes and stabilization of the quadruplex structure.
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| Cell Assay |
A typical protocol for photodynamic therapy: Cells (e.g., HeLa, MCF-7) are seeded in culture plates and incubated with H2TMpyP-2 (1-20 uM) for 4-24 hours. The medium is replaced, and cells are irradiated with visible light (400-700 nm) at a fluence of 1-10 J/cm2. After 24-48 hours, cell viability is measured by MTT assay. Control cells are kept in the dark to assess dark toxicity.
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| Animal Protocol |
In animal studies, mice bearing subcutaneous tumors are injected intravenously with H2TMpyP-2 (0.5-5 mg/kg in PBS). After a drug-to-light interval (typically 4-24 hours), the tumor is illuminated with a laser or LED source (wavelength 400-700 nm, fluence 50-200 J/cm2). Tumor volumes are measured every 2-3 days for 2-4 weeks. Key endpoints include tumor regression, survival, and histology.
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| ADME/Pharmacokinetics |
PK properties of porphyrin photosensitizers: H2TMpyP-2 has a plasma half-life of approximately 2-6 hours in rodents, with preferential accumulation in tumors, liver, spleen, and kidneys. It is excreted primarily via the hepatobiliary system. Formulation is typically in PBS or saline with pH adjustment to 7.4 to ensure solubility.
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| Toxicity/Toxicokinetics |
Toxicity of H2TMpyP-2 is primarily associated with skin photosensitivity. In the absence of light, the compound has low dark toxicity (IC50 > 50 uM in most cell lines). At therapeutic doses, systemic toxicity is mild. However, patients and animals must be protected from direct light exposure for several days post-treatment. The compound is for research use only.
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| References | |
| Additional Infomation |
H2TMpyP-2 chloride is a versatile research tool in both cancer biology and nucleic acid chemistry. Its Captisol-TMPyP complex can be used in supramolecular nanosynthesis to increase singlet oxygen production, enhance photostability, and improve photosensitizing activity. It is also used as a fluorescent probe for DNA and as a standard in porphyrin chemistry.
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| Molecular Formula |
C44H38CL4N8
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|---|---|
| Molecular Weight |
820.64
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| Exact Mass |
818.197
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| CAS # |
129051-18-9
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| Appearance |
Brown to black solid powder
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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. |
| 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 | 1.2186 mL | 6.0928 mL | 12.1856 mL | |
| 5 mM | 0.2437 mL | 1.2186 mL | 2.4371 mL | |
| 10 mM | 0.1219 mL | 0.6093 mL | 1.2186 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.
Products are for research use only; We do not sell to patients
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