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Overview
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Background
Tandutinib (MLN518, CT53518) is a novel, selective and small-molecule inhibitor of FLT3 with IC50 value of 0.22μM [1].Tandutinib (MLN518) has been reported to inhibit FLT3, PDGFR and c-Kit in in vitro kinase assays with IC50 values of 0.22μM, 0.20μM and 0.17μM, respectively. In addition, Tandutinib (MLN518) has been revealed to inhibit wild-type FLT3 or W51 tyrosine phosphorylation with an IC50 value of 30–100 nM. Furthermore, Tandutinib (MLN518) has shown the cell antiproliferation of the FLT3-ITD-positive cells （Molm-13 and Molm-14 cells） with an IC50 value of 10 nM, whereas the FLT3-ITD-negative cells ( THP-1, KG-1, and RS4 cells) were resistant, requiring 1000-fold higher concentrations to inhibit cell growth [1]
[1] Kelly LM1, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM, Williams I, Amaral SM, Curley DP, Duclos N, Neuberg D, Scarborough RM, Pandey A, Hollenbach S, Abe K, Lokker NA, Gilliland DG, Giese NA. CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 2002 Jun;1(5):421-32.
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