Enitociclib

Overview

Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor ( IC 50 =3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II . Enitociclib specifically depletes key short-lived proteins such as c-MYC , MCL-1 and induces tumor cell apoptosis . Enitociclib also interferes with the production of enhancer RNAs ( eRNA ) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib ( HY-10227 ), Lenalidomide ( HY-A0003 ), Pomalidomide ( HY-10984 ), Venetoclax ( HY-15531 ) and Paclitaxel ( HY-B0015 ), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma.

Application

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Product Information

• Catalog No.: HY-103019
• CAS No.: 1610408-97-3
• Molecular Formula: C19H18F2N4O2S
• Molecular Weight: 404.43
• Purity: 99.89%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
• Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
• Availability: In-stock

Source

Original product source