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. Nr.: 2841750-32-9
- Formel: C17H14ClN3O
- Molecular Weight:311.77
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PDE3A |
SLFN12 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.30 nM
|
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.
|
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.
Chemical Information
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CAS. Nr. 2841750-32-9
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Molecular Weight 311.77
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)