化学名称 : AC220/AC-220
CAS : 950769-58-1
英文名称: AC220/AC-220
英文同义词: N-(5-TERT-BUTYLISOXAZOL-3-YL)-N'-[4-[7-(2-MORPHOLIN-4-YLETHOXY)IMIDAZO[2,1-B][1,3]BENZOTHIAZOL-2-YL]PHENYL]UREA
溶解度:Unknown
储存条件:at -20℃ 2 years
生物活性
AC220 is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ± 0.3 nM and >10 mM for MC4-11 and A375, respectively. It exhibits low nanomolar potency in biochemical and cellular assays and exceptional kinase selectivity, and in animal models is efficacious at doses as low as 1 mg/kg given orally once daily. The data reveal that the combination of excellent potency, selectivity, and pharmacokinetic properties is unique to AC220, which therefore is the first drug candidate with a profile that matches the characteristics desirable for a clinical FLT3 inhibitor.
参考文献
[1] Zarrinkar PP et a. Blood. 2009 Oct 1;114(14):2984-92