FLT3-IN-17

FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FAK

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

IC50: 12 nM (FAK), <0.5 nM (D835Y)[2].

FLT3-IN-17 (compound 25, 72 h) inhibits cell growth in HCT-116, MDA-MB-231, A375 cells[1]. FLT3-IN-17 (10 μM) inhibits cytochrome P450s (CYPs) with inhibition rates >55%[1]. FLT3-IN-17 inhibits FLT3 mutants activity (IC50s: <0.5 nM for D835Y, 1.6-183 nM for Ba/F3)[1]. Cell Proliferation Assay[1] Cell Line: HCT-116, MDA-MB-231, A375 cells Concentration: 0-1 μM approximately Incubation Time: 72 h Result: Inhibited cell growth with IC50 values of 0.25, 0.46, 0.49 μM respectively.

[1]. Hanna Cho, et al. Identification of Thieno[3,2- d]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3. J Med Chem. 2021 Aug 26;64(16):11934-11957.