ADH-6
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].
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- No. CAS: 2227429-65-2
- Fòrmula: C29H36N8O9
- Peso molecular:640.64
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Help & FAQs
Actividad biológica
ADH-6 (25 μM, 10 h) inhibits aggregation of pR248W (indicated by dot blot assay)[1].
ADH-6 (5 μM, 6 h) dissociates intracellular mutant p53 aggregates in MIA PaCa-2 cells[1].
ADH-6 (0-10 μM, 24 or 48 h) causes selective cytotoxicity in cancer cells bearing mutant p53 (MIA PaCa-2)[1].
ADH-6 (5 μM, 24 h) specifically targets and reactivates aggregation-prone mutant p53 in MIA PaCa-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA PaCa-2 (mutant R248W p53), SK-BR-3 (mutant R175H p53)
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Concentration:0, 2.5, 5, 7.5, 10 μM
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Incubation Time:24, 48 h
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Result:Caused death of cancer cells bearing mutant, but not WT, p53.
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Cell Line:MIA PaCa-2 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Increased expression of p53-inducible MDM2 and proapoptotic Bax.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MIA PaCa-2 xenografts[1]
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Dosage:716.4 µM in 0.02% DMSO
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Administration:Intraperitoneal injection, every 2 days, for a total of 12 doses
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Result:Reduced tumor growth relative to the saline-treated control group.
Reduced mutant p53 levels and shrinked xenografts harboring aggregation-prone mutant p53.
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Animal Model:MIA PaCa-2 xenografts (pharmacokinetics assay)[1]
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Dosage:15 mg/kg
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Administration:Intraperitoneal injection, for a single dose
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Result:Cmax: 21 µg/mL, T1/2: 3.6 h
Chemical Information
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No. CAS 2227429-65-2
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Peso molecular 640.64
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Fòrmula C29H36N8O9
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SMILES
O=C(C1=NC(OCCCN)=C(NC(C2=NC(OCCCN)=C(NC(C3=NC(OCCCC)=C([N+]([O-])=O)C=C3)=O)C=C2)=O)C=C1)OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ADH-6 Related Classifications
HY-145785 Related Classifications
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