FLT3/CDK4-IN-1
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.
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- CAS. Nr.: 2762296-44-4
- Formel: C25H28F2N8
- Molecular Weight:478.54
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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CDK4 7 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11, HCT-116, MDA-MB-436[1]
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Concentration:Various concentrations
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Incubation Time:72 hours
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Result:FLT3/CDK4-IN-1 had better cell antiproliferative activities against MV4-11and HCT-116 cells, with IC50 of 70 and 100 nM respectively.
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Cell Line:MV4-11, HCT-116[1]
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Concentration:12.5, 25, 50, 100 and 200 nM
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Incubation Time:24 hours
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Result:Arrested the cell cycle in G1 phase in a concentration-dependent manner.
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Cell Line:MV4-11, HCT-116[1]
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Concentration:200, 400, 800, 1600 and 3200 nM
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Incubation Time:48 hours
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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.
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Cell Line:MV4-11[1]
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Concentration:0, 5, 10, 20, 40, 100 nM
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Incubation Time:2 hours
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Result:Inhibited the phosphorylation of FLT3 at Tyr589/591 in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nu/nu mice (MV4-11-injected)[1]
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Dosage:100 and 200 mg/kg
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Administration:p.o.; 14 days, once daily
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Result:Significantly inhibited the tumor growth at the dose of 200 mg/kg while no significant antitumor effect at 100 mg/kg.
Chemical Information
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CAS. Nr. 2762296-44-4
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Molecular Weight 478.54
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Formel C25H28F2N8
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SMILES
CC(N1N=CC2=NC=C(C3=NC(NC4=CC=C(N5CCN(CC)CC5)C(F)=C4)=NC=C3F)C=C21)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
FLT3/CDK4-IN-1 Related Classifications
HY-115904 Related Classifications
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