Antitumor photosensitizer-5
Antitumor photosensitizer-5 (Ru2) is a photosensitizer which effectively target tumor mitochondria with an IC50 of 0.3 μM for phototoxicity to A549 cells. Under 460 nm light irradiation, antitumor photosensitizer-5 induces the generation of reactive oxygen species and NADH depletion, causes mitochondrial damage and activation of caspase-3, inducing apoptosis and suppressing cell migration. Antitumor photosensitizer-5 has the potential to prevent the growth of malignant tumors, therefore, shows the potential to be applied to photodynamic therapy.
For research use only. We do not sell to patients.
- Formula: C53H43F12N11O2P2RuS
- Molecular Weight:1289.04
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Nicotinamide adenine dinucleotide (NADH)[1]
Antitumor photosensitizer-5 (10 μM, 4 h) causes a significant increase (32.08-fold) in fluorescence signal in A549 cells (biotin receptor-positive) while inducing BHK cells (biotin receptor-negative) to exhibit negligible fluorescence increase (7.35-fold)[1].
Antitumor photosensitizer-5 (0.391-100 μM, 24 h) exhibits phototoxicity in both BHK cells and A549 cells and reveals minimal cytotoxicity in the absence of light with over 75 % cell viability under 100 μM[1].
Antitumor photosensitizer-5 (10 μM, 4 h) has a Pearson colocalization coefficient of 0.87 with the mitochondrial probe Mito-Tracker Green[1].
Antitumor photosensitizer-5 (0.15-0.6 μM, 24 h) with 460 nm light irradiation for 15 min exhibits a concentration-dependent reduction in the mitochondrial membrane potential probe fluorescence intensity ratio which indicated the mitochondrial damage, while the ROS probe fluorescence intensity exhibits a concentration-dependent increase, indicating effective generation of ROS [1].
Antitumor photosensitizer-5 (0.15-0.6 μM, 24 h) causes the occurrence of apoptosis in A549 cells after light irradiation, while the apoptosis level is virtually unchanged under dark condition, light condition also causes the increase of activated caspase-3, the migration and damage of DNA and the reduction of cellular NADH content[1].
Antitumor photosensitizer-5 (0.15-0.6 μM, 24 h/48 h) inhibits the cell migration of A549 cells under 460 nm light [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BHK, A549
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Concentration:0.195, 0.391, 0.781, 1.563, 3.125, 6.250, 12.5, 25, 50, 100 μM
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Incubation Time:4 h in dark + 15 min in light or dark + 20 h in dark
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Result:Exhibited phototoxicity in both BHK cells and A549 cells, but was more phototoxic in A549 cells (A549 cell viability < 40% under 0.391 μM while BHK cell viability < 40% under 6.25 μM), revealed minimal cytotoxicity in the absence of light with over 75 % cell viability under 100 μM.
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Cell Line:A549
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Concentration:0.15, 0.3, 0.6 μM
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Incubation Time:4 h in dark + 15 min in light or dark + 20 h in dark
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Result:Increased the percentage of early and late apoptotic cells in A549 in a concentration-dependent manner under the 460 nm light condition. Conversely, under dark conditions, the percentage of early and late apoptotic cells in treated A549 cells remained virtually unchanged.
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Cell Line:A549
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Concentration:0.15, 0.3, 0.6 μM
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Incubation Time:4 h in dark + 15 min in light or dark + 20 h/44 h in dark
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Result:Displayed a significant concentration-dependent inhibition of wound healing in A549 cells under 460 nm light compared to cells kept in the dark.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude female mice (6–8 weeks old) , Human lung adenocarcinoma epithelial A549 cells[1]
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Dosage:10 mg/kg
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Administration:intratumoral injection (i.tu.) for once
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Result:Suppressed the tumor growth remarkably in the light group while tumors in the dark or control groups grow rapidly during the same period.
Caused severe apoptosis and disruption of the tumor structure in the tumor of light group while the tumors in the other group showed no obvious tissue damage, normal organs such as the heart, liver, spleen, lung, and kidney did not exhibit significant pathological abnormalities or inflammatory lesions.
Chemical Information
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Molecular Weight 1289.04
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Formula C53H43F12N11O2P2RuS
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SMILES
O=C(CCCCC1SCC2NC(NC21)=O)NC3=CC=C(C(N4)=NC5=C4C(C=CC=[N]67)=C6C8=C5C=CC=[N]8[Ru+2]9%107([N]%11=C%12C(C=CC%13=C%12[N]%10=CC=C%13)=CC=C%11)[N]%14=CC=CC%15=C%14C%16=[N]9C=CC=C%16C=C%15)C=C3.[F-][P+5]([F-])([F-])([F-])([F-])[F-].[F-][P+5]([F-])([F-])([F-])([F-])[F-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Antitumor photosensitizer-5 Related Classifications
HY-163034 Related Classifications
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- Antitumor photosensitizer-5
- Antitumor photosensitizer5
- Antitumor photosensitizer 5
- Apoptosis
- Reactive Oxygen Species (ROS)
- A549 cell
- MDAMB-231 cell
- MCF-7 cell
- BHK cells
- BALB/c nude mice
- singlet oxygen
- reactive oxygen species
- NADH
- cancer
- mitochondria
- Ruthenium(II) complexes
- Aggregation-induced emission
- caspase-3
- Photodynamic therapy
- Inhibitor
- inhibitor
- inhibit