TBBS-CPT
TBBS-CPT is a photoactivatable prodrug that selectively accumulates in biotin receptor-positive tumor cells. TBBS-CPT responds to glutathione to break disulfide bonds, releasing Camptothecin (HY-16560) and TBBS, which exert a synergistic anticancer effect. Upon light irradiation under both normoxic and hypoxic conditions, TBBS-CPT generates ROS, including superoxide anion radicals. TBBS-CPT preferentially accumulates in mitochondria. TBBS-CPT can be used in cancer-related research.
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- Formule: C68H62IN7O12S4
- Masse moléculaire:1424.42
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Stockage:
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
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
TBBS-CPT undergoes GSH-mediated cleavage to release CPT and TBBS in a cell-free PBS buffer system, and exhibits highly sensitive and selective fluorescent responses to GSH at concentrations ranging from 0 to 100 μM[1].
TBBS-CPT (5.0 μM; 0-60 min) is selectively taken up by biotin receptor-positive 4T1 cancer cells and preferentially localizes to the mitochondria of 4T1 cells[1].
TBBS-CPT produces both type I (O2•-) and type II (1O2) reactive oxygen species synchronously upon white light irradiation, and displays equivalent reactive oxygen species generation efficiency under normoxic and hypoxic environments[1].
TBBS-CPT (0-15 μM; 25 mW/cm2) exhibits potent synergistic chemo-photodynamic cytotoxicity against 4T1 cells, with an IC50 value of 1.54 μM under normoxic conditions and 2.05 μM under hypoxic conditions; its cytotoxicity decreases against biotin-pretreated 4T1 cells (IC50 = 13.47 μM), and its toxicity to NIH-3T3 normal fibroblasts is negligible[1].
TBBS-CPT (5.0 μM; imaged at 0-10 min post-white light irradiation) induces time-dependent mitochondrial dysfunction in 4T1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:4T1 mouse breast cancer cells, biotin-pretreated 4T1 cells, NIH-3T3 normal fibroblasts
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Concentration:0, 0.1, 0.5, 1, 5, 10, 15 μM
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Incubation Time:25 mW/cm2
white light irradiation (cytotoxicity assessment)
dark incubation (dark toxicity assessment) -
Result:Inhibited 4T1 cell viability with an IC50 of 1.54 μM under normoxic conditions with light irradiation; the combination index (CI) was below 1 at concentrations above 0.40 μM, demonstrating synergistic chemo-photodynamic effects.
Reduced sensitivity in biotin-pretreated 4T1 cells, with an IC50 of 13.47 μM.
Inhibited 4T1 cell viability with an IC50 of 2.05 μM under hypoxic conditions with light irradiation.
Showed negligible toxicity to NIH-3T3 cells, and low dark toxicity to 4T1 cells.
Resulted in near-complete 4T1 cell death after treatment with light irradiation, even under hypoxic conditions, as shown by Calcein-AM/PI staining.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 1424.42
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Formule C68H62IN7O12S4
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SMILES
O=C(CCCC[C@H]1SC[C@](N2)([H])[C@@]1([H])NC2=O)OC3=CC(N(C4=CC=CC=C4)C5=CC=CC=C5)=CC=C3/C=C(C#N)/C6=CC=C(C7=CC=[N+](CCOC(OCCSSCCOC(O[C@]8(CC)C(OCC9=C8C=C%10N(CC%11=CC(C=CC=C%12)=C%12N=C%11%10)C9=O)=O)=O)=O)C=C7)S6.[I-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TBBS-CPT Related Classifications
HY-187192 Related Classifications
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