BX912 CAS NO.702674-56-4

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Purity:: 98%

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Product Details

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

ProName: BX912
CasNo: 702674-56-4
Molecular Formula: C20H23BrN8O
Appearance: light yellow solid
Application: CAS：702674-56-4；1-PYRROLIDINECARBOXAMI...
DeliveryTime: 4weeks
PackAge: 100g,500g,1kg,25kg/drum
Port: shang hai
ProductionCapacity: 1 Gram/Week
Purity: 98%
Storage: Dry seal
Transportation: shipping
LimitNum: 100 Milligram

Superiority

we are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.

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our research team of scientists consists of western-trained ph.d.s with experience and capabilities in drug r&d methodologies and medicinal chemistry.

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。

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