AZD4573 hydrochloride (C09-1504-765)

Information:AZD4573 is a potent inhibitor ofCDK9(IC50 of <0.004 μM) with fast-off binding kinetics (t1/2= 16 min) and high selectivity versus other kinases, including other CDK family kinases.Targets:CDK9 <0.004 μM:In vitro:Short-term treatment with AZD4573 leads to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 0.0137 μM in an acute myeloid leukemia model MV4-11). In human cancer cell line panel screens, AZD4573 demonstrates the ability to induce rapid caspase activation (6h) and loss of viability (24h) across a diverse set of hematological cancers (median caspase EC50 = 30 nM, GI50 = 11 nM) but with minimal effect on solid tumors (median EC50 & GI50 >30 μM).In vivo:AZD4573 exhibits a short half-life in multiple preclinical species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration. Specification: 0.98 Molecular Formula: C22H28ClN5O2(free) Molecular Weight: 429.94(free) PubChem CID: 124155204 Isomeric SMILES: CC(=O)N[C@@H]1CCC[C@@H](C1)C(=O)NC2=NC=C(C(=C2)C3=C4CC(CN4N=C3)(C)C)Cl