1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK
  2. CDK FLT3
  3. 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 CDK4IC50 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。

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FLT3/CDK4-IN-1 Chemical Structure

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
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.

纯度 & 产品资料
参考文献
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产品名称:
FLT3/CDK4-IN-1
目录号:
HY-115904
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