JAK2/FLT3-IN-1 (C007B-363094)

JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC 50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2 , FLT3 , JAK1 and JAK3 , respectively. JAK2/FLT3-IN-1 has anti-cancer activityIn VitroJAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner. JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells. JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MV4-11 and SET-2 cells Concentration: 0.008, 0.04, 0.2, 1 μM Incubation Time: For 2 hours Result: Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM. Apoptosis AnalysisCell Line: MV4-11 cells Concentration: 5, 10, 50, 100 nM Incubation Time: For 2 hours Result: Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells. Cell Cycle AnalysisCell Line: MV4-11 cells Concentration: 5, 10, 50, 100 nM Incubation Time: For 2 hours Result: Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM.In VivoJAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) exhibits significant antitumor effects . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD/SCID mouse models Dosage: 30 and 60 mg/kg Administration: Oral administration; daily; for 14 days Result: Exhibited significant antitumor effects. The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model.Form:SolidIC50& Target:JAK2 0.7 nM (IC 50 ) FLT3 4 nM (IC 50 ) JAK1 26 nM (IC 50 ) JAK3 39 nM (IC 50 ). Molecular Formula: C25H34FN7O Molecular Weight: 467.58