Antitumor agent-22
Antitumor agent-22 is an inhibitor of topoisomerase I and II. Antitumor agent-22 can serve as a ROS-responsive prodrug, in which the boronate ester unit undergoes cleavage under the high ROS tumor microenvironment to release the active parent core, thereby inhibiting Top1/Top2. Antitumor agent-22 induces apoptosis in HCT116 cells and triggers G2 phase cell cycle arrest. Antitumor agent-22 exhibits antitumor activity in HCT116 xenograft mouse models in vivo. Antitumor agent-22 can be used for colon cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 2415259-07-1
- Formula: C33H33BFN3O6
- Molecular Weight:597.44
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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
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Topoisomerase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
Topoisomerase I |
Topoisomerase II |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.016 μM
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Antiproliferative activity against human HCT116 cells assessed as viability reduction by CCK8 assay.
Antiproliferative activity against human HCT116 cells assessed as viability reduction by CCK8 assay.
|
32292547 |
| MCF7 | IC50 |
0.033 μM
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Antiproliferative activity against human MCF-7 cells assessed as viability reduction by CCK8 assay.
Antiproliferative activity against human MCF-7 cells assessed as viability reduction by CCK8 assay.
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32292547 |
| A549 | IC50 |
0.037 μM
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Antiproliferative activity against human A549 cells assessed as viability reduction by CCK8 assay.
Antiproliferative activity against human A549 cells assessed as viability reduction by CCK8 assay.
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32292547 |
In Vitro
Antitumor agent-22 releases the parent compound in response to H2O2 in PBS, with a release rate of 11.6% at 0.05 mM H2O2[1].
Antitumor agent-22 exhibits potent antiproliferative activity against HCT116 colon cancer cells with an IC50 of 16 nM[1].
Antitumor agent-22 undergoes intracellular ROS-triggered cleavage in HCT116 cells, first converting to 15a and then to 1a within 8-72 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0.05, 0.2, 0.4 μM
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Incubation Time:48 h
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Result:Induced apoptosis in HCT116 cells.
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Cell Line:HCT116 cells
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Concentration:0.05, 0.2, 0.4 μM
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Incubation Time:24 h
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Result:Induced G2 phase cell cycle arrest in HCT116 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Multiplex immunofluorescence IHC
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- Multiplex immunohistochemistry
- Protocol for Cell Cycle
- Research Protocol for Cancer Immunology
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 2415259-07-1
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Molecular Weight 597.44
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Formula C33H33BFN3O6
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SMILES
O=C(OCC1=CC=C(B2OC(C)(C(C)(C)O2)C)C=C1)OC3=CC4=C(NC5=C4CCN6C(C7=CC(F)=CC=C7N(C56)C)=O)C=C3
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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)
Antitumor agent-22 Related Classifications
HY-133566 Related Classifications
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