HP590 (C09-1138-660)

HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC 50 =27.8 nM; ATP inhibition: IC 50 =24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis.Appearance:SolidIC50& Target:IC50: 27.8 nM (STAT3 luciferase activity)In Vitro:HP590 (0-40 μM; 72 h) shows anti-proliferative activities to MKN45, AGS, and MGC803 cells. HP590 (0-40 nM; 0-24 h) inhibits STAT3 Tyr 705 and Ser 727 phosphorylation in GC cells, blocks the expression of STAT3 downstream genes (c-Myc and cyclin D1) iIn Vivo:HP590 (oral administration; 25 and 50mg/kg; once daily; 5 w) inhibits GC growth effectively by inhibiting the STAT3 activation and shows better tolerance in GC xenograft model. MCE has not independently confirmed the accuracy of these methods. TheyBiological Activity:HP590 is an orally active, novel and potent STAT3 inhibitor (STAT3 luciferase activity: IC 50 =27.8 nM; ATP inhibition: IC 50 =24.7 nM). HP590 shows anti-proliferative activity to gastric cancer cells and induces apoptosis. Specifications and Purity: 98%. Molecular Formula: C29H24F6N4O3. Molecular Weight: 590.52.