| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
The Golgi apparatus (GA) proteins, eukaryotic translation initiation factor 2-alpha (eIF2α) kinase 3 (EIF2AK3) and protein Disulfide isomerase A3 (PDIA3), as well as Golkin subfamily A member 2 (GOLGA2), galactosyltransferase 1 (GALT1), and several other GA proteins are reduced in abundance when photodynamic therapy (PDT) combined with redaporfin (5μM) is applied. Conversely, there was no discernible decrease in the cytoskeletal protein β-actin or the mitochondrial import receptor component TOM20 homolog (TOMM20) [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Human osteosarcoma U2OS cells Tested Concentrations: 0.3, 0.6, 1.3, 2.5, 5, 10 μM Incubation Duration: 6 hrs (hours) Experimental Results: Induced GBF1, GOLGA2 and GALT1 abundance diminished such as EIF2AK3 and PDIA3. |
| References | |
| Additional Infomation |
Redaporfin is a bacteriochlorin-based photosensitizer, with antineoplastic activity upon photodynamic therapy (PDT). Following intravenous administration, redaporfin preferentially accumulates in hyperproliferative tissues, such as tumors. Local application of laser light at the tumor site results in the absorption of light by this agent and a photodynamic reaction between LUZ 11 and oxygen. This results in the production of reactive oxygen species (ROS), which includes singlet oxygen molecules, the superoxide ion, and other cytotoxic free radicals. The formation of ROS induces free radical-mediated DNA damage and cell death.
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| Exact Mass |
1134.156
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|---|---|
| CAS # |
1224104-08-8
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| PubChem CID |
86287614
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| Appearance |
Brown to black solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.617
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| LogP |
11.24
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
76
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| Complexity |
2150
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C([H])C(=C(C=1F)C1=C2C([H])=C([H])C(=C(C3=C(C([H])=C([H])C(=C3F)S(N([H])C([H])([H])[H])(=O)=O)F)C3C([H])([H])C([H])([H])C(=C(C4=C(C([H])=C([H])C(=C4F)S(N([H])C([H])([H])[H])(=O)=O)F)C4=C([H])C([H])=C(C(C5=C(C([H])=C([H])C(=C5F)S(N([H])C([H])([H])[H])(=O)=O)F)=C5C([H])([H])C([H])([H])C1=N5)N4[H])N=3)N2[H])F)(N([H])C([H])([H])[H])(=O)=O |c:11,17,46,t:94|
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| InChi Key |
CKRVBMUJCFKRND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C48H38F8N8O8S4/c1-57-73(65,66)33-17-5-21(49)37(45(33)53)41-25-9-11-27(61-25)42(38-22(50)6-18-34(46(38)54)74(67,68)58-2)29-13-15-31(63-29)44(40-24(52)8-20-36(48(40)56)76(71,72)60-4)32-16-14-30(64-32)43(28-12-10-26(41)62-28)39-23(51)7-19-35(47(39)55)75(69,70)59-3/h5-9,11,14,16-20,57-61,64H,10,12-13,15H2,1-4H3
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| Chemical Name |
2,4-difluoro-N-methyl-3-[10,15,20-tris[2,6-difluoro-3-(methylsulfamoyl)phenyl]-2,3,12,13,22,24-hexahydroporphyrin-5-yl]benzenesulfonamide
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| Synonyms |
F2BMet LUZ 11 LUZ11F-2BMet LUZ-11 F 2BMet
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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 |
| 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 : ~100 mg/mL (~88.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02070432 | UNKNOWN STATUS | Drug: LUZ11 | Head and Neck Cancer | Luzitin SA | 2014-02 | Phase 1 Phase 2 |
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