CasNo.702674-56-4,BX912,(702674-56-4) Suppliers

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Keywords

BX912 702674-56-4 1-PYRROLIDINECARBOXAMIDE, N-[3-[[5-BROMO-4-[[2-(1H-IMIDAZOL-4-YL)ETHYL]AMINO]-2-PYRIMIDINYL]AMINO]PHENYL]-;BX 912;PYRROLIDINE-1-CARBOXYLIC ACID (3-(5-BROMO-4-[2-(1H-IMIDAZOL-4-YL)-ETHYLAMINO]-PYRIMIDI

Quick Details

Appearance:light yellow solid
Application:CAS：702674-56-4；1-PYRROLIDINECARBOXAMIDE, N-[3-[[5-BROMO-4-[[2-(1H-IMIDAZOL-4-YL)ETHYL]AMINO]-2-PYRIMIDINYL]AMINO]PHENYL]-;BX 912;PYRROLIDINE-1-CARBOXYLIC ACID (3-(5-BROMO-4-[2-(1H-IMIDAZOL-4-YL)-ET
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ProductionCapacity:1|Gram|Week
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Details:

BX-912

生物活性体外研究

中文名称:	BX-912
中文同义词:	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
英文名称:	BX-912
英文同义词:	1-PYRROLIDINECARBOXAMIDE, N-[3-[[5-BROMO-4-[[2-(1H-IMIDAZOL-4-YL)ETHYL]AMINO]-2-PYRIMIDINYL]AMINO]PHENYL]-;BX 912;PYRROLIDINE-1-CARBOXYLIC ACID (3-(5-BROMO-4-[2-(1H-IMIDAZOL-4-YL)-ETHYLAMINO]-PYRIMIDIN-2-YLAMINO)-PHENYL)-AMIDE;N-[3-[[5-Bromo-4-[[2-(1H-imidazol-5-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide;BX912/BX-912;N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide;BX-912 N-[3-[[5-Bromo-4-[[2-(1H-imidazol-5-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide;N-[3-[[5-Bromo-4-[[2-(1H-imidazol-5-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-912
CAS号:	702674-56-4
分子式:	C20H23BrN8O
分子量:	471.35
EINECS号:
相关类别:	Inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1).;信号转导通路激酶抑制剂;小分子抑制剂;Inhibitors;小分子抑制剂，天然产物
Mol文件:	702674-56-4.mol

BX-912 性质

密度

1.596

BX-912 用途与合成方法

生物活性

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。

体外研究

BX912 抑制ChcK1,PKA,c-kit,和KDR，IC50分别为0.83, 0.11, 0.85, 和0.41 μM。BX912 作用于肿瘤细胞，阻断PDK1/Akt信号，在培养中也抑制多种肿瘤细胞的贴壁依赖型生长(比如PC-3细胞)或者诱导凋亡。许多癌细胞系(比如MDA-468乳腺癌)具有提高的Akt活性，在软琼脂中培养的组织对BX912的敏感性比在组织培养塑料上高30多倍, 和PDK1/Akt信号通路的细胞生存一致，这对没有粘附的细胞尤其重要。BX912 有效抑制PDK1酶活, 但是不抑制AKT2活性(IC50>10 μM)。因此, BX-912是PDK1的直接抑制剂。BX912是PDK1 活性的竞争性抑制剂，BX912 结合到PDK1的ATP结合袋中。BX912的氨基嘧啶骨架采用与PDK1激活位点相似的位点。BX912显著提高的含4 N DNA的MDA-468 细胞数, 且使细胞停在 G2/M期。BX912也有效抑制HCT-116细胞生长，按1 μM剂量处理抑制率达96%。BX912有效抑制细胞生长，IC50为0.32μM。