FLT3-IN-36
FLT3-IN-36 is a potent FLT3 inhibitor. FLT3-IN-36 exhibits antitumor activity against FLT3-mutated acute myeloid leukemia (AML) cells. FLT3-IN-36 induces cell cycle arrest, reduces mitochondrial membrane potential, and induces apoptosis, downregulating FLT3 and downstream protein expression (including AKT, ERK, PI3K, and STAT5). FLT3-IN-36 can be used for AML research.
For research use only. We do not sell to patients.
- Formula: C21H17NO3
- Molecular Weight:331.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
FLT3-IN-36 (compound 8h) (24 h) exhibits selective antiproliferative activity against FLT3 mutant AML cells, with IC50s of 2.04 (MV4-11) and 3.25 μM (MOLM-13), while showing significantly weaker effects on FLT3 wild-type cells such as THP-1, U937, and OCI-AML2 (IC50 = 19.59, 91.49, and 55.38 μM)[1].
FLT3-IN-36 (0.1-100 μM, 24 h) inhibits MV4-11 cell growth in a time- and dose-dependent manner, while showing low cytotoxicity in normal HK-2 and HepRG cells[1].
FLT3-IN-36 (1-10 μM, 24 h) induces apoptosis, G2/M phase cell cycle arrest and a reduction of mitochondrial membrane potential in MV4-11 cells in a dose-dependent manner[1].
FLT3-IN-36 (0-10 μM, 24 h) inhibits the growth of MV4-11 cells by by downregulating FLT3 protein levels and inactivating its downstream signaling pathway, including key effectors such as AKT, ERK, PI3K, and STAT5[1].
FLT3-IN-36 fits well to the ATP binding pocket of FLT3 and only interacts with the residues Glu692 and Cys694 in the hinge region of the active conformation[1].
FLT3-IN-36 (1-10 μM) directly targets FLT3 kinase, exhibiting 58% inhibition of FLT3-ITD kinase activity at 10 μM[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:1, 2.5 and 5 μM
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Incubation Time:24 h
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Result:Significantly increased the G2/M phase arrest in MV4-11.
Induced the G2/M phase arrest at moderate concentration with a dose-dependent manner after treatment for 24 h.
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Cell Line:MV4-11, HK-2 and HepRG cells
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Concentration:0.1, 1, 2, 4, 8, 10, 16, 50, and 100 μM
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Incubation Time:24 and 48 h
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Result:Decreased MV4-11 cell viability in a time- and dose-dependent manner.
Showed low cytotoxicity in normal HK-2 and HepRG cells.
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Cell Line:MV4-11 cells
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Concentration:0, 2.5, 5, and 10 μM
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Incubation Time:24 h
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Result:Promoted the cleavage and activation of Caspase-3 (evidenced by increased levels of cleaved Caspase-3).
Resulted in no obvious changes for the levels of Bcl-2 and Bax.
Caused the decrease of the downstream-related protein levels, including AKT, ERK, PI3K and STAT5.
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Cell Line:MV4-11 cells
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Concentration:1, 2.5 and 5 μM
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Incubation Time:24 h
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Result:Induced apoptosis in MV4-11 cells with a dose-dependent manner.
Chemical Information
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Molecular Weight 331.36
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Formula C21H17NO3
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SMILES
O=C(C1CC1)C2=CC(C(C3=C(C(C)=O)C=CC=C3)=O)=C4C=CC=CN42
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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)