产品
编 号:F756997
分子式:C27H35F4N7O3
分子量:581.61
产品类型
结构图
CAS No: 2928093-29-0
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产品详情
生物活性:
JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 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 (TFA) has anti-cancer activity.
体内研究:
JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects.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.
体外研究:
JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner.JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) 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) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells.