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.
For research use only. We do not sell to patients.
- Formula: C27H29N5O
- Molecular Weight:439.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50 value of 16.0 nM against FLT3-ITD and an IC50 value of 20.4 nM against FLT3-D835Y[1]
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.
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Cell Line:MV4-11 cells
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Concentration:2 μM
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Incubation Time:24 h
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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%.
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Cell Line:MV4-11 cells
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Concentration:0.2 μM, 2 μM, 5 μM
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Incubation Time:24 h
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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.
Chemical Information
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Molecular Weight 439.55
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Formula C27H29N5O
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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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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)