中文名: | Quizartinib (AC220);奎扎替尼 |
中文别名: | N-(5-叔丁基异恶唑-3-基)-N‘-{4-[7-[2-(吗啉-4-基)乙氧基]咪唑并[2,1-b][1,3]苯并噻唑-2-基]苯基}脲;AC-220; AC220 |
英文名称: | Quizartinib (AC220) |
英文别名: | N-(5-tert-Butylisoxazol-3-yl)-N‘-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea |
CAS No.: | 950769-58-1 |
分子式: | C29H32N6O4S |
分子量: | 560.67 |
性状: | 属性溶解性DMSO 33.2 mg/mL; Water<0.3 mg/mL; Ethanol <0.5 mg/mL存贮条件储存温度-20°C描述产品介绍Quizartinib (AC220)是一种二代FLT3抑制剂,作用于Flt3(ITD/WT),IC50为1.1 nM/4.2 nM,作用于Flt3比作用于KIT, PDGFRA, PDGFRB, RET,和CSF-1R选择性高10倍。Phase 3。用途An Flt-3/Flk-2 inhibitor.生化机理Quizartinib, Free Base, is an fms-related tyrosine kinase 3 (FLT3) receptor tyrosine kinase inhibitor. In binding assays, quizartinib has demonstrated a high affinity for FLT3 (Kd = 1.6 nM). in vitro assays examining FLT3 internal tandem duplicate mutations and wild-type FLT3 demonstrate the ability of quizartinib to inhibit FLT3 autophosphorylation (IC50 = 1.1 nM for FLT3-ITD and 4.2 nM for wt FLT3). Quizartinib, Free Base, has also been shown to inhibit the growth of human leukemia cell line MV4-11 (IC50 = 0.56 nM) and A375 cells (IC50 > 10,000 nM). |
储存: | 储存温度-20°C |
安全术语: | |
风险术语: | |
危险品标志: | |
危险品运输编号: | |
用途: | 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. [1][2] |