1. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling PI3K/Akt/mTOR MAPK/ERK Pathway Apoptosis
  2. FLT3 STAT Akt ERK Apoptosis
  3. 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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FLT3-IN-41

FLT3-IN-41 Chemical Structure

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Description

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[1].

IC50 & Target

STAT5

 

In Vitro

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.

Cell Cycle Analysis[1]

Cell Line: FLT3-ITD mutant MV4-11 cells
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: 24 h
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.

Real Time qPCR[1]

Cell Line: FLT3-ITD mutant MV4-11 cells
Concentration: 400 nM
Incubation Time: 0 h, 2 h, 24 h
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.
Molecular Weight

469.45

Formula

C26H19N3O6

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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
FLT3-IN-41
Cat. No.:
HY-182281
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