产品
编 号：F755657
分子式：C25H28F2N8
分子量：478.54
分子式：C25H28F2N8
分子量：478.54
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CAS No: 2762296-44-4
产品详情
生物活性：
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.
体内研究：
FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg.Animal Model:Female nu/nu mice (MV4-11-injected)
Dosage:100 and 200 mg/kg
Administration:p.o.; 14 days, once daily
Result:Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.
体外研究：
FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner.FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116.FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo.
体内研究：
FLT3/CDK4-IN-1 (100 and 200 mg/kg; p.o.; 14 days, once daily) significantly inhibits the tumor growth at the dose of 200 mg/kg.Animal Model:Female nu/nu mice (MV4-11-injected)
Dosage:100 and 200 mg/kg
Administration:p.o.; 14 days, once daily
Result:Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.
体外研究：
FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner.FLT3/CDK4-IN-1 (200-3200 nM; 48 hours) induces apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and is more capable in MV4-11 than HCT-116.FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.
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