AZD 5438 is an antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1/cyclin B1 (IC50 = 16 nM), Cdk2/cyclin E (IC50 = 6 nM), Cdk2/cyclin A (IC50 = 45 nM), Cdk6/cyclin D3 (IC50 = 21 nM), and Cdk9/cyclin T (IC50 = 20 nM). AZD5438 also inhibits the kinase activity of p25-cdk5 (IC50 = 14 nM) and glycogen synthase kinase 3β (IC50 = 17 nM). AZD5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates, and exhibits the broad antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50 ranging from 0.2 μM (MCF-7) to 1.7 μM (ARH-77).
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Soluble in DMSO (100 mM), water (<1 mg/ml) at 25 °C, and ethanol (74 mg/ml) at 25 °C.
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