702674-56-4BX-912

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商品编号：B126138

库存现货：9

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商品名称：702674-56-4BX-912
商品毛重：0.00
单位：件
上架时间：2017-10-31 22:54:30

名称: BX-912英文名称: BX-912≥97%产品编号 B126138
CAS号: 702674-56-4分子式 C₂₀H₂₃BrN₈O分子量471.36
Beilstein号 EC号 MDL号 PubChem编号

属性

存贮条件	储存温度-20°C

描述

产品介绍	BX-912是一种有效的，特异性的PDK1抑制剂，IC50为12 nM，作用于PKD1比作用于PKA和PKC选择性分别高9和105倍。
别名	N-[3-[[5-溴-4-[[2-(1H-咪唑-5-基)乙基]氨基]-2-嘧啶基]氨基]苯基]-1-吡咯烷甲酰胺;BX912;BX 912;N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
生化机理	BX-912 is a PDK-1 inhibitor. BX 912 suppresses growth in a number of cell lines and also induces apoptosis. Cell lines with elevated levels of AKT are >30-fold more sensitive to PDK1 inhibition by BX-912. This compound is a competitive inhibitor of PDK1, indicating that it binds to the ATP-binding pocket to inhibit phosphorylation. BX-912 accomplishes this due to the fact that the aminopyrimidine backbone, which adopts a similar conformation to ATP in the active site of PDK1. BX-912 potently inhibits the growth of PC-3 cells in soft agar, displaying an IC50 of 320 nM.
备注	BX912 is a potent and specific PDK1 inhibitor with IC50 of 12 nM, 9- and 105- fold greater selectivity for PKD1 than PKA and PKC, respectively. In comparison to GSK3β, selectivity for PDK1 is 600-fold.
应用	A potent and selective PDK-1 inhibitor that induces apoptosis