FLT3-IN-28
Product Specifications
Target
STAT, Apoptosis, FLT
Related Pathways
Angiogenesis, Stem Cells, Tyrosine Kinase/Adaptors, JAK/STAT signaling, Apoptosis
Bioactivity
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13/14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.
Smiles
C1C(CN1C(=O)NC2=NC=CC(=C2)OC3=C(C=C(C=C3)NC(=O)C4=CN(N=N4)C5=CN=CC=C5)F)O
Molecular Formula
C23H19FN8O4
Molecular Weight
490.447
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
Frequently Asked Questions
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