CHMFL-FLT3-122

CHMFL-FLT3-122 is a **potent and selective small molecule inhibitor** of the FLT3 receptor tyrosine kinase, with an IC50 of 40 nM for FLT3 and over 10-fold selectivity over BTK kinase and 170-fold selectivity over c-KIT. It was discovered through structure-guided drug design aimed at targeting FLT3-ITD mutant, which is implicated in approximately 30% of acute myeloid leukemia (AML) cases. CHMFL-FLT3-122 inhibits the proliferation of FLT3-ITD positive AML cell lines, induces apoptosis, and causes cell cycle arrest at G0/G1 phase. It has shown oral bioavailability (~30%) and demonstrated antitumor efficacy in FLT3-ITD positive AML xenograft models without significant toxicity. It is being studied as a potential targeted therapy, particularly for FLT3-ITD positive AML[1][2][3][4][5][7][9].

Other names

CHMFL-FLT3-122CHMFL-FLT-3-122CHMFL-FLT 3-122HYML-122HYML122HYML 122TR122TR-122TR 122