| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Talaporfin targets cancer cells through photodynamic therapy. Upon activation with light, it generates reactive oxygen species (ROS), leading to localized cell damage and tumor destruction. It induces apoptosis, DNA double-strand breaks, and ROS production.
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|---|---|
| ln Vitro |
In vitro, talaporfin sodium acts as a photosensitizer that, upon light activation, generates ROS and induces cell death. It kills all tumor cells in the targeted zone, rather than only the minority of cells undergoing rapid division.
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| ln Vivo |
Advice (This is our suggested procedure; it should be adjusted to suit your particular requirements; it is merely a guide) [1]. Inside labeling: 1. produced by injecting reconstituted tumor cells into the brain's frontal lobe 2. Talaporfin sodium is administered intravenously at a dose of 5 mg/kg body weight; the concentration of talaporfin sodium is 5 mg/1 ml, or 0.9% saline. 3. creation of a brain model tumor. Jordan received an intraperitoneal injection of 5-ALA at a dose of 100 mg/kg body weight. The concentration of 5-ALA in the injection was 20 mg/ml of 0.9% normal saline. 4. Obtain the 5 mm thick brain tissue specimen that corresponds to the tumor (or edema). 5. Use 1 ml of 100% dimethyl sulfoxide (DMSO) to fully homogenize the sample, then add an aliquot of 100 μL of the supernatant. into each of the 96-well plate's wells. 6. Measure the sample's relative fluorescence intensity at an emission wavelength of 670±10 nm using a microplate reader. The relative fluorescence intensity (au) per 1 g of sample weight was used to standardize the sample's relative fluorescence intensity.
In vivo, talaporfin sodium is used in photodynamic therapy for various cancers. It accumulates in tumor tissues and, upon light activation, induces localized cell damage and tumor destruction. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for talaporfin are not typically performed as it is a photosensitizer rather than a enzyme inhibitor. Its photodynamic activity is evaluated by measuring ROS production and cell killing upon light activation.
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| Cell Assay |
For in vitro cell-based assays, talaporfin sodium is dissolved in aqueous buffers and applied to cultured cancer cells at concentrations ranging from 0.1-10 µM. Cells are then exposed to light at 664 nm, and effects on cell viability, apoptosis, and ROS production are assessed.
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| Animal Protocol |
Animal/Disease Models: Rat brain tumor model [1]
Doses: 5 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: High fluorescence intensity and retention were shown in brain tumors that were distinguished from vasogenic edema. In vivo animal studies commonly use mouse xenograft models. Talaporfin sodium is administered intravenously at doses ranging from 1-10 mg/kg. Tumors are then exposed to light at 664 nm, and anti-tumor efficacy is evaluated by measuring tumor volume and histopathology. |
| ADME/Pharmacokinetics |
Talaporfin sodium has a molecular weight of 799.69 g/mol and a molecular formula of C38H37N5Na4O9. It is a water-soluble PDT photosensitizer.
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| Toxicity/Toxicokinetics |
Talaporfin sodium has a manageable toxicity profile. Photosensitivity is a potential side effect. No significant systemic toxicity has been reported at therapeutic doses.
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| References | |
| Additional Infomation |
LS11 (tarapofen sodium) is a photosensitizing drug composed of chlorophyll-derived chlorhexidine e6 and L-aspartic acid. Upon intratumoral activation via a light-emitting diode (LED), tarapofen sodium forms a high-energy conformation, generating singlet oxygen, which leads to free radical-mediated cell death. It is used to treat various cancers.
Tarapofen sodium is a photosensitizing drug composed of chlorophyll-derived chlorhexidine e6 and L-aspartic acid. Upon intratumoral activation via a light-emitting diode (LED), tarapofen sodium forms a high-energy conformation, generating singlet oxygen, which leads to free radical-mediated cell death. (NCI04) Drug Indications Under investigation for the treatment of macular degeneration. Mechanism of Action Light Sciences Oncology (LSO) is dedicated to bringing light to cancer patients. Light Sciences has developed a novel treatment for solid tumors called photoinfusion therapy (Litx). This therapy first involves implanting a flexible light-emitting diode (LED) into the tumor, followed by the injection of the photoactivated drug LS11 (tarapophen sodium). Once the LED activates LS11, molecular oxygen is converted into singlet oxygen, killing tissue within the LED's irradiation range and blocking blood supply to the area. This therapy is suitable for three types of cancer: liver cancer, metastatic colorectal cancer, and glioma (brain tumor). Talaporfin sodium is a second-generation photosensitizer that has shown promising results in clinical trials for the treatment of various cancers. It is used in photodynamic therapy (PDT). |
| Molecular Formula |
C38H37N5NA4O9
|
|---|---|
| Molecular Weight |
799.69
|
| Exact Mass |
799.218
|
| CAS # |
220201-34-3
|
| Related CAS # |
220201-34-3 (sodium);110230-98-3 (free acid);
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| PubChem CID |
5488036
|
| Appearance |
Purple to black solid powder
|
| Boiling Point |
1175.5ºC at 760mmHg
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| Flash Point |
664.7ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
56
|
| Complexity |
1340
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
CCC1=C(C2=CC3=C(C(=C(N3)C=C4[C@H]([C@@H](C(=N4)C(=C5C(=C(C(=N5)C=C1N2)C)C(=O)[O-])CC(=O)N[C@@H](CC(=O)[O-])C(=O)[O-])CCC(=O)[O-])C)C)C=C)C.[Na+].[Na+].[Na+].[Na+]
|
| InChi Key |
JLWROAPZCOJYGT-OBJGRMLXSA-J
|
| InChi Code |
InChI=1S/C38H41N5O9.4Na/c1-7-20-16(3)24-12-26-18(5)22(9-10-32(45)46)35(42-26)23(11-31(44)41-30(37(49)50)15-33(47)48)36-34(38(51)52)19(6)27(43-36)14-29-21(8-2)17(4)25(40-29)13-28(20)39-24;;;;/h7,12-14,18,22,30,39-40H,1,8-11,15H2,2-6H3,(H,41,44)(H,45,46)(H,47,48)(H,49,50)(H,51,52);;;;/q;4*+1/p-4/t18-,22-,30-;;;;/m0..../s1
|
| Chemical Name |
tetrasodium;(2S)-2-[[2-[(2S,3S)-7-carboxylato-3-(2-carboxylatoethyl)-17-ethenyl-12-ethyl-2,8,13,18-tetramethyl-2,3,23,24-tetrahydroporphyrin-5-yl]acetyl]amino]butanedioate
|
| 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, 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)
|
| Solubility (In Vitro) |
H2O : ~25 mg/mL (~31.26 mM)
DMSO : ~2 mg/mL (~2.50 mM) |
|---|---|
| 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 | 1.2505 mL | 6.2524 mL | 12.5048 mL | |
| 5 mM | 0.2501 mL | 1.2505 mL | 2.5010 mL | |
| 10 mM | 0.1250 mL | 0.6252 mL | 1.2505 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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