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Cat. No.: HY-187192

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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.

For research use only. We do not sell to patients.

Formula: C₆₈H₆₂IN₇O₁₂S₄
Molecular Weight:1424.42

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

TBBS-CPT Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
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References
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Biological Activity

Description

In Vitro

OthersOxidative StressAnti-cancerMitochondrial Function

Others

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].

Oxidative Stress

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].

Anti-cancer

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].

Mitochondrial Function

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.

Cell Cytotoxicity Assay^[1]

Cell Line:

4T1 mouse breast cancer cells, biotin-pretreated 4T1 cells, NIH-3T3 normal fibroblasts
Concentration:

0, 0.1, 0.5, 1, 5, 10, 15 μM
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

Anti-cancer

TBBS-CPT (1 mM; 150 μL; i.v.; single dose; with white LED irradiation; 14 days) exerts significantly enhanced tumor inhibition in 4T1 tumor-bearing BALB/c mice relative to treatment with TBBS-CPT alone, PBS, or CPT, with no observed body weight loss^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

ROS/oxidative-stress fluorescent staining

Chemical Information

Molecular Weight 1424.42
Formula C₆₈H₆₂IN₇O₁₂S₄
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-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu Z, et al. Tumor-targeted activatable molecular agent for synergistic chemo-photodynamic therapy. Bioorganic chemistry. 2026 Sep 15;180:110199. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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