1. Cell Cycle/DNA Damage
    Protein Tyrosine Kinase/RTK
  2. CDK
    FLT3
  3. FLT3/CDK4-IN-1

FLT3/CDK4-IN-1 

Cat. No.: HY-115904
Handling Instructions

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.

For research use only. We do not sell to patients.

FLT3/CDK4-IN-1 Chemical Structure

FLT3/CDK4-IN-1 Chemical Structure

CAS No. : 2762296-44-4

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Description

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)

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.
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.
Molecular Weight

478.54

Formula

C25H28F2N8

CAS No.
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Product Name:
FLT3/CDK4-IN-1
Cat. No.:
HY-115904
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