| 应用 |
An Flt-3/Flk-2 inhibitor. |
| 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。 |
| 备注 |
Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 1/2. |
| 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). |
| 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;N-(5-tert-Butylisoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea |
