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AZD3229
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD3229图片
CAS NO:2248003-60-1
规格:98%
分子量:479.51
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
AZD3229是一种有效的、广泛的突变型酪氨酸激酶受体(KIT)抑制剂,可用于开发治疗胃肠道间质瘤。
CAS:2248003-60-1
分子式:C24H26FN7O3
分子量:479.51
纯度:98%
存储:Store at -20°C

Background:

AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.


AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM). AZD3229 Tosylate demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR can be rationalised predominantly by the interaction of water molecules with the protein and ligand in the active site and its kinome selectivity is similar to the best of the approved GIST agents[1].



[1]. Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy) quinazolin-4-yl]amino} phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct 11;61(19):8797-8810.