FLT3-IN-12 is a selective and orally bioavailable inhibitor of the FLT3 kinase, demonstrating IC50 values of 1.48 nM for FLT3-WT and 2.87 nM for the FLT3-D835Y mutant. This compound exhibits exceptional selectivity over c-KIT, surpassing 1000-fold. Additionally, FLT3-IN-12 showcases potent anti-acute myeloid leukemia (AML) activity, with an IC50 of 0.75 nM against the MV4-11 cell line, making it a valuable tool for the study of FLT3-driven malignancies and potential therapeutic applications in AML.
FLT3-IN-12 is a selective and orally bioavailable inhibitor of the FLT3 kinase, demonstrating IC50 values of 1.48 nM for FLT3-WT and 2.87 nM for the FLT3-D835Y mutant. This compound exhibits exceptional selectivity over c-KIT, surpassing 1000-fold. Additionally, FLT3-IN-12 showcases potent anti-acute myeloid leukemia (AML) activity, with an IC50 of 0.75 nM against the MV4-11 cell line, making it a valuable tool for the study of FLT3-driven malignancies and potential therapeutic applications in AML.
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