Antitumor agent-100
Antitumor agent-100 is an orally active molecular glue that promotes the PDE3A-SLFN12 interaction and induces cell death. Antitumor agent-100 binds to the catalytic pocket of PDE3A, extends hydrophobic groups to mediate the hydrophobic interaction between PDE3A and SLFN12, and stabilizes the PDE3A-SLFN12 complex. Antitumor agent-100 induces cancer cell apoptosis and inhibits tumor growth in mouse xenograft models. Antitumor agent-100 can be used for the research of cervical cancer.
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- CAS No.: 2841750-32-9
- Formule: C17H14ClN3O
- Masse moléculaire:311.77
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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
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PDE3A |
SLFN12 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.30 nM
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Induction of apoptosis against human HeLa cells assessed as reduced cellular ATP levels after 36 h incubation by cell viability assay.
Induction of apoptosis against human HeLa cells assessed as reduced cellular ATP levels after 36 h incubation by cell viability assay.
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34707099 |
In Vitro
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 athymic (nu/nu) nude mice (female, 4 weeks old, 18-20 g, subcutaneous HeLa cell inoculation)[1]
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Dosage:1-5 mg/kg
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Administration:p.o.; once daily for 8 days then twice daily for 6 days
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Result:Achieved dramatic tumor growth inhibition, with tumor volume decreasing to near 0 by day 15 at 5 mg/kg.
Produced significant tumor volume reduction compared to the vehicle group at 1 mg/kg.
Caused no bodyweight reduction in either treatment group.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- 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. 2841750-32-9
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Masse moléculaire 311.77
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Formule C17H14ClN3O
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SMILES
O=C1N=C2NC3=C(CN2C1)C(Cl)=C(C4=CC=C(C)C=C4)C=C3
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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)
Antitumor agent-100 Related Classifications
HY-153802 Related Classifications
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