FLT3/CDK4-IN-1 是一种有效的、高选择性且具有口服活性的FLT3/CDK4双重抑制剂 (FLT3 与 CDK4 的IC50为 7 和 11 nM)。FLT3/CDK4-IN-1 对某些癌细胞具有抗增殖活性，在体内具有良好的抗肿瘤作用。

FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3 / CDK4 dual inhibitor ( IC 50 =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 [1].

FLT3/CDK4-IN-1 (compound 23k) (various concentrations; 72 hours) has better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC 50 of 70 and 100 nM respectively [1]. FLT3/CDK4-IN-1 (12.5-200 nM; 24 hours) arrests the cell cycle in G1 phase in a concentration-dependent manner [1]. 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 [1]. FLT3/CDK4-IN-1 (0-100 nM; 2hours) inhibits the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner [1]. Cell Proliferation Assay Cell Line: MV4-11, HCT-116, MDA-MB-436 [1] Concentration: Various concentrations Incubation Time: 72 hours Result: FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC 50 of 70 and 100 nM respectively. Cell Cycle Analysis Cell Line: MV4-11, HCT-116 [1] Concentration: 12.5, 25, 50, 100 and 200 nM Incubation Time: 24 hours Result: Arrested the cell cycle in G1 phase in a concentration-dependent manner. Apoptosis Analysis Cell Line: MV4-11, HCT-116 [1] Concentration: 200, 400, 800, 1600 and 3200 nM Incubation Time: 48 hours Result: Induced apoptosis in both MV4-11 and HCT-116 cells with concentration dependent manner, and was more capable in MV4-11 than HCT-116. Western Blot Analysis Cell Line: MV4-11 [1] Concentration: 0, 5, 10, 20, 40, 100 nM Incubation Time: 2 hours Result: Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.

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 [1]. Animal Model: Female nu/nu mice (MV4-11-injected) [1] 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.

2762296-44-4

C25H28F2N8

478.54

(< 1 mg/ml refers to the product slightly soluble or insoluble )
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