Quizartinib
Cat. No.:YN430145
产品名称: | Quizartinib |
CAS No.: | 950769-58-1 |
Chemical Name: | N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]-urea |
Synonyms: | 奎扎替尼; AC220 |
分子量: | 560.67 |
分子式: | C₂₉H₃₂N₆O₄S |
SMILES: | O=C(NC1=NOC(C(C)(C)C)=C1)NC2=CC=C(C=C2)C3=CN4C(SC5=CC(OCCN6CCOCC6)=CC=C45)=N3 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Quizartinib (AC220) 是一种具有口服活性的、高选择性的,有效的第二代 Ⅱ 型 FLT3(type II FLT3)酪氨酸激酶抑制剂,Kd值为 1.6 nM。Quizartinib 抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化,IC50分别为 4.1 nM 和 1.1 nM。Quizartinib 可以通过优化的 linker 与 VHL 配体连接,从而形成 PROTAC Flt3 降解剂。Quizartinib 诱导细胞凋亡 (apoptosis)。 |
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Chao, Q., Sprankle, K.G., Grotzfeld, R.M., 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) inhibitorJ. Med. Chem.52(23),7808-7816(2009)
Zarrinkar, P.P., Gunawardane, R.N., Cramer, M.D., et al.AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)Blood114(14),2984-2992(2009)