FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC . FLT3/HDAC-IN-3 potently inhibits FLT3 ( IC 50 = 14 nM), HDAC1 ( IC 50 = 27 nM), HDAC6 ( IC 50 = 20 nM), and FLT3 D853Y ( IC 50 = 55 nM), exhibits weak activity against HDAC8 , and shows no activity against HDAC4 . FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies.
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