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.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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.
Protocole
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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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