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Biological Activity:
A uniquely potent, selective and efficacious inhibitor of FMS-Like Tyrosine kinase-3 (FLT3) for the treatment of AML; Second-generation FLT3 inhibitor that is highly potent with low nanomolar potency both in vitro and in cellular assays, and has a highly focused and selective interaction pattern across the human protein kinome.
References:
PP Zarrinkar et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 2009, 114 (14), 2984-2992. [online]
PH Wiernik. FLT3 inhibitors for the treatment of acute myeloid leukemia. Clin. Adv. Hematol. Oncol. 2010, 8(6), 429-444. [online]
Q Chao et al. Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. J. Med. Chem. 2009, 52(23), 7808-7816. [online]
Chemical Name: N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride
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