FLT3/CDK4-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

FLT3/CDK4-IN-1 

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

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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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[1].

IC50 & Target

CDK4

7 nM (IC50)

体外研究
(In Vitro)

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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 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.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

478.54

Formula

C25H28F2N8
CAS 号

2762296-44-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Li X, et al. Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors. Bioorg Chem. 2022;121:105669.

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