FLT3-IN-28
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation) . Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD[1].
Product Specifications
UNSPSC
12352005
Target
Apoptosis; FLT3; STAT
Related Pathways
Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Field of Research
Cancer
Smiles
O=C(N1CC(O)C1)NC2=CC(OC3=CC=C(NC(C4=CN(C5=CC=CN=C5)N=N4)=O)C=C3F)=CC=N2
Molecular Formula
C23H19FN8O4
Molecular Weight
490.45
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
STAT5
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