JAK2/FLT3-IN-3 (11r) is a dual inhibitor of FLT3 and JAK2, with IC50 values respectively at 0.51 nM for FLT3, 2.01 nM for JAK2, and 104.40 nM for JAK3. It can induce apoptosis and exhibits anticancer activity.

FLT3:0.51 nM, JAK3:104.40 nM, JAK2:2.01 nM

JAK2/FLT3-IN-3 (11r) exhibits potent antiproliferative activity across various cancer cell lines, including HEL (IC 50 = 1.1 μM), MV4-11 (IC 50 = 9.43 nM), RPMI-8226 (IC 50 = 0.793 μM), NCI-H929 (IC 50 = 0.743 μM), Ba/F3-FLT3-ITD-D835Y (IC 50 = 0.099 μM), and Ba/F3-FLT3-ITD-F691L (IC 50 = 0.042 μM). These results demonstrate its strong antiproliferative effects in a range of cell lines.

JAK2/FLT3-IN-3 (11r) demonstrates moderate absorption in rats with a peak concentration (Cmax) of 38.7 ng/mL and an area under the curve (AUC) of 522 ng·h/mL. The maximum concentration is reached at 5.33 hours (Tmax), and the oral bioavailability is calculated at 25.2%.