TBP-EQ
TBP-EQ is a cationic aggregation-induced emission photosensitizer and luminogen that enables bright red aggregation-state fluorescence imaging. TBP-EQ generates reactive oxygen species (ROS) via Type I/II pathways under light irradiation. TBP-EQ undergoes light-triggered translocation from the plasma membrane to mitochondria, enhancing penetration and mitochondrial enrichment, and induces oxidative plasma membrane damage, increased permeability, as well as mitochondrial oxidative stress, dysfunction, and depolarization. TBP-EQ exhibits photodynamic cytotoxicity against breast cancer cells, and intratumoral injection followed by light activation inhibits tumor growth. TBP-EQ preferentially accumulates in breast cancer cells and prolongs tumor retention while reducing off-target fluorescence. TBP-EQ can be used for breast cancer-related research.
For research use only. We do not sell to patients.
- Formula: C43H49N3O2S
- Molecular Weight:671.93
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
3.44 μM
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Photocytotoxicity against murine 4T1 cells assessed by CCK-8 assay after white-light irradiation at 100 mW/cm2 for 10 min.
Photocytotoxicity against murine 4T1 cells assessed by CCK-8 assay after white-light irradiation at 100 mW/cm2 for 10 min.
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42691882 |
In Vitro
TBP-EQ (60 min) has a maximum absorption wavelength of 491 nm and retains >90% absorbance after white light irradiation[1].
TBP-EQ (5.0 μM) generates ROS under 100 mW/cm2 white light via Type I and Type II photodynamic pathways, with a relative 1O2 generation efficiency of 232% that of Rose Bengal[1].
TBP-EQ (5 s-30 min) preferentially accumulates in 4T1 breast cancer cells rather than NIH-3T3 fibroblasts, with 2.3-fold higher intracellular accumulation[1].
TBP-EQ (5 μM) localizes to the plasma membrane of 4T1 cells[1].
TBP-EQ (5 μM; 30 min pre-incubation) undergoes light-triggered redistribution from the plasma membrane to mitochondria in 4T1 cells[1].
TBP-EQ (0-5 μM; 10 min) has an IC50 of 3.44 μM and slightly decreases 4T1 cell viability under light exposure[1].
TBP-EQ (5.0 μM; 0-90 s) produces time-dependent intracellular ROS in 4T1 cells under white light irradiation[1].
TBP-EQ (5.0 μM; pre-incubation for 30 min followed by irradiation for 10 min) plus light exposure induces mitochondrial depolarization and ultrastructural damage 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 cells
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Concentration:0, 1, 2, 3, 4 and 5 μM
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Incubation Time:10 min (white-light irradiation at 100 mW/cm2); 0, 5, and 10 min (Live/Dead irradiation)
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Result:Both compounds exhibited negligible dark cytotoxicity up to 5 μM.
Upon light irradiation, this compound induced concentration-dependent phototoxicity toward 4T1 cells with a fitted IC50 of 3.44 μM.
At 5 μM, approximately 7% of 4T1 cells survived after this compound exposure under light irradiation.
Live/Dead staining showed nearly complete cell death, with dominant red fluorescence.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c[1]
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Dosage:5 μM, 100 μL per 200 mm3 tumor; white light 100 mW/cm2
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Administration:intratumoral injection (i.t.); once every 3 days for 3 cycles; white light irradiation 2 h after injection
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Result:On day 14, the compound + light group achieved a tumor inhibition rate of 97.5%; the compound alone group had a tumor inhibition rate of 3.8%.
Suppressed tumor growth, with some instances of tumor regression.
H&E staining of tumors from the compound + light group showed extensive regions of apoptotic and necrotic cells; tumors from the compound alone group displayed abundant viable tumor cells with intact morphology.
- How to Select the Route of Administration for Mammals
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- ROS/oxidative-stress fluorescent staining
- Patient-Derived Xenograft (PDX)
- Transepithelial/transendothelial electrical resistance assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Bioluminescent/Fluorescent Imaging Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Molecular Weight 671.93
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Formula C43H49N3O2S
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SMILES
CC[N+](CC)(CC)CCOCCOCC[N+](C=C1)=CC=C1C(C2=CSC=C32)=CC=C3C(C=C4)=CC=C4N(C5=CC=CC=C5)C6=CC=CC=C6
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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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TBP-EQ Related Classifications
HY-189567 Related Classifications
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