AZD4573 hydrochloride - 98%, high purity , CAS No.2057509-72-3(free), Inhibitor of cyclin dependent kinase 9

Item Number

A414132

• Synonyms: E5XSP3X68B | s8719 | (1S,3R)-N-(5-chloro-4-{5,5-dimethyl-4H,5H,6H-pyrrolo[1,2-b]pyrazol-3-yl}pyridin-2-yl)-3-acetamidocyclohexane-1-carboxamide | HY-112088 | BA166454 | AZD 4573 [WHO-DD] | AS-871/40187168 | NSC816554 | (1S,3R)-3-Acetamido-N-(5-chloro-4-(5
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t_1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of cyclin dependent kinase 9

Product Description

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.