FLT3-IN-14 

FLT3-IN-14 is a potent FLT3 inhibitor with IC₅₀s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model^[1].

IC₅₀: 1.4 nM (FLT-ITD), 5.6 nM (FLT3-WT)^[1]

FLT3-IN-14 (compound 9c) (0-10 μM; 24 hours) inhibits the proliferation of tested twelve haematological cell lines with IC₅₀s of 0.011-1.582 μM^[1].
FLT3-IN-14 (0-10 μM; 72 hours) exhibits low toxicity, with GI₅₀ greater than 10 μM, in resting lymphocytes^[1].
FLT3-IN-14 (1-50 nM; 24 and 48 hours) accumulates annexin-V positive cells in a concentration and time-dependent manner^[1].
FLT3-IN-14 (25-100 nM; 24 and 48 hours) induces a significant G1 arrest in both cell lines^[1].
FLT3-IN-14 (1-50 nM; 24 hours) induces the dephosphorylation of FLT3^[1].

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

FLT3-IN-14 (1.0 and 3.0 mg/kg; IP; daily for 28 days) significantly reduces tumor growth in a dose-dependent manner without sign of toxicity^[1].

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

472.56

C₂₅H₂₄N₆O₂S

2620551-45-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Cilibrasi V, Spanò V, Bortolozzi R, et al. Synthesis of 2H-Imidazo[2',1':2,3] [1,3]thiazolo[4,5-e]isoindol-8-yl-phenylureas with promising therapeutic features for the treatment of acute myeloid leukemia (AML) with FLT3/ITD mutations. Eur J Med Chem. 2022  [Content Brief]