Inhibition of STAT5 phosphorylation in human SET2 cells xenografted in SCID mouse assessed as tumor growth inhibition at 50 mg/kg, po as single dose measured up to 12 hrs post treatment
Inhibition of STAT3 phosphorylation in human SET2 cells xenografted in SCID mouse assessed as tumor growth inhibition at 50 mg/kg, po as single dose measured up to 12 hrs post treatment
Inhibition of STAT5 phosphorylation in human SET2 cells xenografted in SCID mouse assessed as tumor growth inhibition at 30 mg/kg, po as single dose measured at 1 to 3 hrs post treatment
Inhibition of STAT3 phosphorylation in human SET2 cells xenografted in SCID mouse assessed as tumor growth inhibition at 30 mg/kg, po as single dose measured at 1 to 3 hrs post treatment
Antitumor activity against human SET2 cells implanted in AML patients assessed as reduction in tumor volume administered intraperitoneally relative to control
Antitumor activity against human SET2 cells xenografted in SCID Beige mouse assessed as tumor growth inhibition at 0.16 mg/kg, ip qd measured on day 33 relative to control
Antitumor activity against human SET2 cells overexpressing JAK2 V617F mutant xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 30 mg/kg, po qd for 18 days measured every 2 days for 18 days by caliper method relative to control
Antitumor activity against human SET2 cells overexpressing JAK2 V617F mutant xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 60 mg/kg, po qd for 18 days measured every 2 days for 18 days by caliper method relative to control
Induction of cell cycle arrest in human SET2 cells assessed as accumulation at G0/G1 phase incubated for 24 hrs by propidium iodide staining based flow cytometry
Antitumor activity against human SET2 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 15 mg/kg, po qd administered for 16 days and measured every 2 days relative to control
Antitumor activity against human SET2 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 30 mg/kg, po qd administered for 16 days and measured every 2 days relative to control
Antitumor activity against human SET2 cells xenografted in NOD/SCID mouse assessed as tumor growth inhibition at 60 mg/kg, po qd administered for 16 days and measured every 2 days relative to control
Induction of apoptosis in human SET-2 cells assessed as necrotic cells at 0.05 uM incubated for 24 hrs by Annexin V/PI staining based flow cytometric analysis (Rvb = 0.78%)