1. Protein Tyrosine Kinase/RTK Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. FLT3 Apoptosis Reactive Oxygen Species (ROS)
  3. FLT3-IN-39

FLT3-IN-39 (Compound W4) is a selective FLT3 inhibitor, with an IC50 value of 16.0 nM against FLT3-ITD and an IC50 value of 20.4 nM against FLT3-D835Y. FLT3-IN-39 inhibits FLT3-ITD and FLT3-D835Y mutant kinases. FLT3-IN-39 induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and reduces intracellular ROS levels. FLT3-IN-39 exhibits anti-tumor activity against acute myeloid leukemia.

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FLT3-IN-39

FLT3-IN-39 Chemical Structure

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Description

FLT3-IN-39 (Compound W4) is a selective FLT3 inhibitor, with an IC50 value of 16.0 nM against FLT3-ITD and an IC50 value of 20.4 nM against FLT3-D835Y. FLT3-IN-39 inhibits FLT3-ITD and FLT3-D835Y mutant kinases. FLT3-IN-39 induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and reduces intracellular ROS levels. FLT3-IN-39 exhibits anti-tumor activity against acute myeloid leukemia[1].

IC50 & Target

IC50 value of 16.0 nM against FLT3-ITD and an IC50 value of 20.4 nM against FLT3-D835Y[1]

In Vitro

FLT3-IN-39 potently inhibits FLT3-ITD (IC50 = 16.0 nM) and FLT3-D835Y (IC50 = 20.4 nM) kinases, while exhibits extremely low activity against c-KIT[1].
FLT3-IN-39 potently inhibits the proliferation of FLT3-ITD-positive MV4-11 cells (IC50 = 0.86 μM), MOLM-13 cells (IC50 = 0.92 μM), as well as the solid tumor cell lines A549, HepG2 and HCT116[1].
FLT3-IN-39 (2 μM; 24 h) induces G0/G1 cell cycle arrest in MV4-11 cells[1].
FLT3-IN-39 (0.2-5 μM; 24 h) induces apoptosis in MV4-11 cells in a concentration-dependent manner[1].
FLT3-IN-39 (0.2-2 μM; 24 h) reduces the intracellular ROS level in MV4-11 cells in a concentration-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Increased the proportion of MV4-11 cells in the G0/G1 phase to 77.48%.
Decreased the proportion of cells in the S phase to 13.73%.
Decreased the proportion of cells in the G2/M phase to 8.8%.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.2 μM, 2 μM, 5 μM
Incubation Time: 24 h
Result: Induced MV4-11 cell apoptosis with a rate of 23.3% at 0.2 μM.
Induced MV4-11 cell apoptosis with a rate of 84.6% at 2 μM.
Induced MV4-11 cell apoptosis with a rate of 92.4% at 5 μM.
Molecular Weight

439.55

Formula

C27H29N5O

SMILES

CN(C1CCN(C)CC1)C2=NC(NC(C=C3)=CC=C3OC4=CC=CC=C4)=C(C=CC=C5)C5=N2

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Room temperature in continental US; may vary elsewhere.

Storage

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-39
Cat. No.:
HY-181945
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