CDDD11-8 is an orally administered, highly potent and selective CDK9 and FLT3-ITD inhibitor, with K i values of 8 nM and 13 nM, respectively. It effectively reduces the proliferation of leukemia cell lines, showing particular efficacy against those with the FLT3-ITD mutation [1] [2].

CDK9:8 nM (Ki)

CDDD11-8 administered orally at doses between 0 to 125 mg/kg daily can induce tumor regression [1]. In an animal model using MV4-11 tumor-bearing mice [1], the compound was tested at dosages of either 75 or 125 mg/kg. The administration was carried out orally on a daily basis for either 5 or 28 days. Results confirmed potent inhibition of CDK9 in vivo, as evidenced by the reduced phosphorylation of RNAPII at Ser2 and Ser5. Moreover, a decrease in the phosphorylation of FLT3 at Tyr591 and STAT5 at Tyr694 was observed, affirming the compound's effectiveness.