JAK2/FLT3-IN-1 has anti-cancer activity. JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively.

JAK2/FLT3-IN-1 (0.005-0.1 μM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells. JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner from 0.008 to 1 μM. JAK2/FLT3-IN-1 (0.005-0.1 μM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells.

JAK2/FLT3-IN-1 exhibits significant antitumor effects and the tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.

2387765-27-5

C25H34FN7O

467.58

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years