(3R,4R)-3-氟-4-羟基吡咯烷-1-羧酸叔丁酯信息二维码

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CAS 1174020-50-8
级别 国标/gb
品牌 macklin
规格 1g
含量 99.0%
管控 2-8°C, 密封, 干燥
库存码 R756682-100mg
分子式 C9H16FNO3
分子量 205.2266
英文名 (3R,4R)-tert-Butyl 3-fluoro-4-hydroxypyrrolidine-1-carboxylate
数量
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库存1mg   起订1mg
 
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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
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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]
[1] Zarrinkar PP et a. Blood. 2009 Oct 1;114(14):2984-92

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