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.
For research use only. We do not sell to patients.
- CAS No.: 2762296-44-4
- Formula: C25H28F2N8
- Molecular Weight:478.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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.
In Vivo
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 No. 2762296-44-4
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Molecular Weight 478.54
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FLT3/CDK4-IN-1 Related Classifications
HY-115904 Related Classifications
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