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Art. -Nr.: HY-183256

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BAY-7728

BAY-7728 is an orally active and selective dual inhibitor of KAT6A (IC₅₀: 45 nM)/KAT6B (IC₅₀: 95 nM). BAY-7728 can effectively inhibit tumor growth and regulate the acetylation level of histone H3K23. BAY-7728 can be used for tumor research.

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CAS. Nr.: 2767642-46-4
Formel: C₂₀H₁₉FN₂O₅S
Molecular Weight:418.44

Speicherung:

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

BAY-7728 Chemical Structure

CAS. Nr.: 2767642-46-4

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Biologische Aktivität
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- In Vitro
- In Vivo
Chemical Information
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Bioz

Biologische Aktivität

Beschreibung

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

BAY-7728 exhibits IC₅₀ values of 55 nM and 164 nM against MVLN and ZR75-1 cells, respectively.

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

In Vivo

BAY-7728 (2.5-100 mg/kg; oral administration; once daily; 22 days) reduces intratumoral H3K23ac levels and inhibits tumor growth in a dose-dependent manner without obvious dose-limiting toxicity in NMRI nude mice bearing LCLC-97TM1 human lung cancer xenografts.

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

Animal Model:

NMRI nude mice bearing established LCLC-97TM1 human lung cancer xenografts
Dosage:

2.5-100 mg/kg
Administration:

Oral, once daily, for 22 consecutive days
Result:

Demonstrated dose-dependent inhibition of tumor growth and reduction of intratumoral histone H3K23 acetylation (H3K23ac) levels in the LCLC-97TM1 xenograft model.
Was well tolerated at all tested doses, with no significant dose-limiting toxicity observed, and increased systemic exposure (AUC) correlated with enhanced antitumor efficacy.

Chemical Information

CAS. Nr. 2767642-46-4
Molecular Weight 418.44
Formel C₂₀H₁₉FN₂O₅S
SMILES

FC1=C2C(OC(C(NS(=O)(C3=CC=CC=C3OCC)=O)=O)=C2)=CC(N4CCC4)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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