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2762296-44-4

2762296-44-4 structure
2762296-44-4 structure
  • Name: FLT3/CDK4-IN-1
  • Chemical Name: FLT3/CDK4-IN-1
  • CAS Number: 2762296-44-4
  • Molecular Formula: C25H28F2N8
  • Molecular Weight: 478.54
  • Create Date: 2022-06-25 16:53:34
  • Modify Date: 2024-01-20 18:23:37
  • 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].

Name FLT3/CDK4-IN-1
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].
Related Catalog
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]. 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]. 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.
References

[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.

Molecular Formula C25H28F2N8
Molecular Weight 478.54