FLT3-IN-41
FLT3-IN-41 is a highly potent FLT3 inhibitor. The IC50 values of FLT3-IN-41 against human FLT3-ITD and FLT3-WT are 3.16 nM and 294.7 nM, respectively. By binding to the ATP-binding pockets of FLT3-ITD and FLT3-WT and forming hydrogen bonds with hinge region residues and Phe830, FLT3-IN-41 inhibits the STAT5, Akt and Erk signaling pathways. FLT3-IN-41 induces G2/M phase arrest and promotes apoptosis in FLT3-ITD-positive acute myeloid leukemia cells, exhibiting significant antiproliferative activity. FLT3-IN-41 serves as a valuable tool for the study of acute myeloid leukemia.
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- Formule: C26H19N3O6
- Masse moléculaire:469.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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STAT5 |
FLT3-IN-41 (compound 35) (1-100 nM; 24 h) induces G2/M cell cycle arrest in FLT3-ITD-mutated MV4-11 cells in a dose-dependent manner[1].
FLT3-IN-41 (1-100 nM; 24 h) induces apoptosis in FLT3-ITD-mutated MV4-11 cells in a dose-dependent manner[1].
FLT3-IN-41 (400 nM; 0-24 h) time-dependently downregulates the mRNA expression levels of STAT5 downstream target genes Osm, Bcl-2, Pim-1 and Cis in FLT3-ITD mutant MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FLT3-ITD mutant MV4-11 cells
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Concentration:1 nM, 10 nM, 100 nM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in the G2/M population in MV4-11 cells.
Resulted in 1.39-, 1.81-, and 3.72-fold increases in the percentage of cells in G2/M phase compared with the untreated controls, respectively.
This effect was distinct from that of midostaurin, which showed different cell cycle arrest patterns in previous reports.
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Cell Line:FLT3-ITD mutant MV4-11 cells
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Concentration:400 nM
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Incubation Time:0 h, 2 h, 24 h
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Result:Significantly reduced the mRNA expression levels of STAT5 transcriptionally regulated genes in a time-dependent manner.
The expression levels of Osm, Bcl-2, Pim-1, and Cis were markedly downregulated after 2 h and 24 h.
Chemical Information
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Masse moléculaire 469.45
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Formule C26H19N3O6
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SMILES
O=C1NC(C2=C1C(C(C=CC=C3)=C3N45)=C4C6=C2C7=C(C=CC=C7)N6[C@H]8[C@H](O)[C@@H](O)[C@H](O)[C@]5(C)O8)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FLT3-IN-41 Related Classifications
HY-182281 Related Classifications
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