AZ20

• CAT Number: I000921
• CAS Number: 1233339-22-4
• Molecular Formula: C₂₁H₂₄N₄O₃S
• Molecular Weight: 412.51
• Purity: ≥95%
• Target: ATM/ATR
• Solubility: DMSO 80 mg/ml; Water <1 mg/ml
• Storage: Store at -20°C
• IC50: 5 nM
• InChI: InChI=1S/C21H24N4O3S/c1-14-13-28-11-10-25(14)19-12-18(21(7-8-21)29(2,26)27)23-20(24-19)16-4-3-5-17-15(16)6-9-22-17/h3-6,9,12,14,22H,7-8,10-11,13H2,1-2H3/t14-/m1/s1
• InChIKey: SCGCBAAYLFTIJU-CQSZACIVSA-N
• SMILES: CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=O)(=O)C)C4=C5C=CNC5=CC=C4

AZ20 (CAT: I000921) is a potent and selective inhibitor of the bromodomain and extra-terminal (BET) family of proteins. BET proteins play a crucial role in gene expression regulation and are involved in various cellular processes, including cancer development and inflammation. AZ20 specifically targets the bromodomains of BET proteins, preventing their interaction with acetylated histones and transcription factors. This inhibition leads to the suppression of oncogenic gene expression and subsequent inhibition of tumor cell growth. AZ20 has shown promising results in preclinical studies, demonstrating antitumor activity in various cancer models, including hematological malignancies and solid tumors.

Reference

1:J Med Chem. 2013 Mar 14;56(5):2125-38. doi: 10.1021/jm301859s. Epub 2013 Mar 1. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.Foote KM,Blades K,Cronin A,Fillery S,Guichard SS,Hassall L,Hickson I,Jacq X,Jewsbury PJ,McGuire TM,Nissink JW,Odedra R,Page K,Perkins P,Suleman A,Tam K,Thommes P,Broadhurst R,Wood C, PMID: 23394205 DOI: 10.1021/jm301859s