FLT3/TrKA-IN-1 

FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC₅₀s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML)^[1].

FLT3/TrKA-IN-1 (compound 4ACP) (1000, 2000, 3000, 4000, 5000 nM; 24, 48, 72 h) shows antiproliferative activity in a concentration and time-dependent pattera with IC₅₀s of 38.8 nM, 54.9 nM for MOLM-13 and MV4-11 cells, respectively^[1].
FLT3/TrKA-IN-1 (500, 1000, 1500, 2000, 2500 nM) dose not elicit cytotoxic activity against GDM-1 and THP-1 AML cell lines which do not carry FLT3-ITD mutation^[1].
FLT3/TrKA-IN-1 shows potent activity against colon cancer KM12 cell line with an GI₅₀ value of 358 nM^[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 24 h, 48 h) inhibits ERK1/2 (extracellular regulated kinases 1/2) and mTOR (mammalian target of rapamycin) in FLT3-ITD positive AML (acute myeloid leukemia) cell lines in a dose-dependent manner^[1].
FLT3/TrKA-IN-1 (0, 10, 50, 100 nM; 72 h) induces cell cycle arrest at the G0/G1 phase as well as apoptosis and necrotic cell death of FLT3-ITD harboring AML cells^[1].
FLT3/TrKA-IN-1 ( 0, 1, 10, 100, 1000 nM; 72 h) dose not elicit drastic cytotoxic effects on BNL and H9c2 cells^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

454.56

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• [1]. Dokla EME, et al. Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. Bioorg Med Chem. 2022; 56:116596.  [Content Brief]