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Background Information:
AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor with a bivalent binding mode. Unlike many previously reported monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously. The enhanced avidity afforded through bivalent binding translates into increased cellular and antitumor activity in preclinical hematologic tumor models. In vivo administration of AZD5153 led to tumor stasis or regression in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. The relationship between AZD5153 exposure and efficacy suggests that prolonged BRD4 target coverage is a primary efficacy driver (ref. 1). AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. Transcriptional modulation of MYC and HEXIM1 was confirmed in AZD5153-treated human whole blood (ref. 1).
Reference:
1. G. W. Rhyasen, et al, AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies, Mol Cancer Ther; 15(11); 2563–74.
2. Robert H. Bradbury, et al, J. Med. Chem., 2016, 59 (17), pp 7801–7817.
APIM050017:AZD5153
CAS No.: 1869912-40-2.
Molecular Formula: C25H33N7O3 ?C11H8O3.
Molecular Weight: 667.8 (or refer to Certificate of Analysis).
Purity: >99% chemical and optical purity by achiral HPLC and chiral HPLCs.
QC: Achiral and Chiral HPLCs, 1H-NMR, Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate.
Storage: Refer to Certificate.
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