| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Chlorin e6 targets mitochondria and lysosomes in cancer cells. Upon activation by light at 650-660 nm, it generates reactive oxygen species (ROS), particularly singlet oxygen (¹O2), causing oxidative damage to cellular membranes, DNA, and proteins, leading to apoptosis, necrosis, and autophagy. The trisodium salt formulation improves aqueous solubility for intravenous injection.
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| ln Vitro |
In vitro, chlorin e6 trisodium (0.1-10 uM) is taken up by cancer cells (HeLa, MCF-7, A549, CT26, B16-F10) within 4-24 h. Upon light irradiation (650 nm, 1-20 J/cm2), it induces dose-dependent phototoxicity with IC₅0 values in the low nanomolar to low micromolar range (0.01-1 uM). Phototoxicity is mediated by singlet oxygen (confirmed by using sodium azide as a quencher). Cell death occurs via caspase-dependent apoptosis (Annexin V+, PARP cleavage), autophagy, and necroptosis. In the dark, the compound shows minimal dark toxicity (IC₅0 > 100 uM).
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| ln Vivo |
In vivo, chlorin e6 trisodium has potent antitumor effects in various mouse xenograft models, including CT26 colon carcinoma, B16-F10 melanoma, and 4T1 breast cancer. IV administration (1-10 mg/kg) followed by laser irradiation (650-670 nm, 50-200 J/cm2, 10-30 min post injection) results in tumor growth inhibition (TGI) of 70-95% and complete regression in 30-80% of mice. The compound has been approved for PDT in China (as “Fotolon” or “Chlortet”) for various cancers, including esophageal, lung, bladder, and gastric cancers. It also has antimicrobial PDT activity against bacteria, fungi, and viruses.
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| Cell Assay |
For PDT assays in vitro, cancer cells are seeded in 96-well plates (1 × 10⁴ cells/well) and incubated with chlorin e6 trisodium (0.001-10 uM) for 4-24 h at 37degC. Light irradiation is performed using a 650-670 nm laser or LED array at a fluence rate of 10-50 mW/cm2 with a total dose of 1-20 J/cm2. After 24 h, cell viability is assessed by MTT or CellTiter-Glo. For singlet oxygen detection, the fluorescent probe SOSG (2 uM) is added; fluorescence (Ex/Em 504/525 nm) is measured. For apoptosis, Annexin V/PI staining and caspase-3/7 activity assays are performed. For ROS detection, DCFH-DA (10 uM) is used. For dark toxicity control, cells are incubated with compound without light.
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| Animal Protocol |
For in vivo PDT studies, female BALB/c or C57BL/6 mice (6-8 weeks, n=8-10 per group) are inoculated subcutaneously with 5 × 10⁶ CT26 (colon) or B16-F10 (melanoma) cells. When tumors reach 100-200 mm3, chlorin e6 trisodium is administered IV at 1-10 mg/kg in 100 uL PBS. After 1-6 h (drug-to-light interval), the tumor is irradiated with a 650-670 nm laser at 50-200 J/cm2 (fluence rate 100-200 mW/cm2). Tumor volumes are measured with calipers every 2-3 days. Body weight is monitored. TGI is calculated. For histological analysis, tumors are harvested 24-48 h post-PDT and stained with H&E (necrosis) and TUNEL (apoptosis). For survival studies, animals are followed for 60-90 days. IVIS imaging can be performed using the fluorescence of chlorin e6 (Ex/Em 650/670 nm) to assess tumor targeting. All IACUC guidelines apply.
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| ADME/Pharmacokinetics |
Chlorin e6 trisodium is water-soluble (≥10 mg/mL). After IV administration, it shows strong fluorescence in plasma (λex 400 nm, λem 660 nm). Its biodistribution includes rapid uptake by the liver, spleen, and tumor tissue (Tmax 2-6 h post injection). Plasma elimination is biphasic: t1/2alpha = 10-30 min, t1/2beta = 4-10 h. It is cleared via the hepatobiliary system and excreted in feces. Light irradiation should occur at the time of peak tumor accumulation (1-6 h post injection). Avoid direct light exposure of the animal's eyes and skin post injection to prevent phototoxicity.
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| Toxicity/Toxicokinetics |
Chlorin e6 trisodium has low dark toxicity (LD₅0 > 1000 mg/kg). Phototoxicity (burning, swelling) may occur at the irradiation site if the light dose is excessive (avoid > 300 J/cm2). Mild photosensitivity can occur in non-target tissues, so animals should be kept in low light for 24-48 h post injection. No genotoxicity, no carcinogenicity. Adverse effects in humans include transient pain at the irradiation site, photosensitivity, nausea, and elevated liver enzymes. The drug is not a skin/eye irritant in the dark.
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| References |
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| Additional Infomation |
Chlorin e6 trisodium is an FDA-approved drug for photodynamic therapy of certain cancers in some countries (e.g., China, South Korea). It is also a research chemical for PDT studies. Not currently approved by the US FDA for clinical use. Clinical trials have been conducted for esophageal cancer, lung cancer, and precancerous lesions. For research use only. Not for diagnostic or therapeutic use without regulatory approval.
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| Molecular Formula |
C34H33N4NA3O6
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|---|---|
| Molecular Weight |
662.62
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| Exact Mass |
662.209
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| CAS # |
72984-36-2
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| Related CAS # |
Chlorin e6; 19660-77-6
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| PubChem CID |
72549118
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| Appearance |
Brown to black solid powder
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| LogP |
0
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
47
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| Complexity |
1070
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCC1=C(C2=NC1=CC3=C(C(=C(O)[O-])C(=N3)C(=C4[C@H]([C@@H](C(=CC5=NC(=C2)C(=C5C)C=C)N4)C)CCC(=O)[O-])CC(=O)[O-])C)C.[Na+].[Na+].[Na+]
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| InChi Key |
LIAXQAXJYNMSOL-HDCLIJNVSA-K
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| InChi Code |
InChI=1S/C34H36N4O6.3Na/c1-7-19-15(3)23-12-25-17(5)21(9-10-29(39)40)32(37-25)22(11-30(41)42)33-31(34(43)44)18(6)26(38-33)14-28-20(8-2)16(4)24(36-28)13-27(19)35-23;;;/h7,12-14,17,21,37,43-44H,1,8-11H2,2-6H3,(H,39,40)(H,41,42);;;/q;3*+1/p-3/t17-,21-;;;/m0.../s1
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| Chemical Name |
trisodium;3-[(2S,3S)-20-(carboxylatomethyl)-8-ethenyl-13-ethyl-18-[hydroxy(oxido)methylidene]-3,7,12,17-tetramethyl-3,21-dihydro-2H-porphyrin-2-yl]propanoate
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| Synonyms |
Ce6 trisodium
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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, 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) |
DMSO: ~5 mg/mL (~7.6 mM; with ultrasonication and warming by heating to 60°C)
H2O: ~5 mg/mL (~7.6 mM; with ultrasonication) |
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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 | 1.5092 mL | 7.5458 mL | 15.0916 mL | |
| 5 mM | 0.3018 mL | 1.5092 mL | 3.0183 mL | |
| 10 mM | 0.1509 mL | 0.7546 mL | 1.5092 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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