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Drug intelligence / Profile preview
AZ960
- Development stage
- Preclinical
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
AZ960 is a potent, selective, and ATP-competitive small-molecule inhibitor of Janus kinase 2 (JAK2), with a Ki of 0.45 nM. Developed by AstraZeneca, AZ960 inhibits the JAK/STAT signaling pathway, specifically blocking STAT5 phosphorylation and downstream transcriptional activation. It has been investigated preclinically for its antiproliferative and apoptotic effects in hematologic malignancies, such as adult T-cell leukemia (ATL) and myeloproliferative neoplasms, as well as in overcoming CDK4/6 inhibitor resistance in estrogen receptor-positive (ER+) breast cancers.
- Other names
- (S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrileAZ 960AZ960AZ-960
02
Targets
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