JAK2-IN-7

459.59

10 mM in DMSO

Protein Tyrosine Kinase/RTK; Epigenetics; Stem Cell/Wnt; JAK/STAT Signaling

JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
In Vitro: JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2V617F cells.

JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase.

JAK2-IN-7 (0.05-1.6 uM; 2 hours) induces apoptosis in SET-2 cells.

In Vivo: JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model.

JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib.