CasNo.1032350-13-2,MK-2206 2HCl,(1032350-13-2) Suppliers

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Keywords

MK-2206 2HCl MK-2206;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride;MK-2206 Dihydrochloride;8-[4-(1-AMinocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f] 1032350-13-2

Quick Details

Appearance:White crystal
Application:CAS：1032350-13-2；MK-2206;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride;MK-2206 Dihydrochloride;8-[4-(1-AMinocyclobutyl)phenyl]-9-phenyl-1,
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ProductionCapacity:1000|Metric Ton|Month
Storage:Dry seal
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Details:

MK-2206 2HCl

生物活性体外研究体内研究特征

中文名称:	MK-2206 2HCl
中文同义词:	8-[4-(1-氨基环丁基)苯基]-9-苯基-1,2,4-三唑并[3,4-F][1,6]萘啶-3(2H)-酮二盐酸盐
英文名称:	MK-2206 2HCl
英文同义词:	MK-2206;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride;MK-2206 Dihydrochloride;8-[4-(1-AMinocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one Hydrochloride;MK-2206 2HCl;8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride MK-2206;MK-2206 8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
CAS号:	1032350-13-2
分子式:	C25H21N5O
分子量:	407.46714
EINECS号:
相关类别:	Amines;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;信号转导通路激酶抑制剂;Inhibitor;新药;PI3K/Akt/mTOR;小分子抑制剂;Inhibitors;小分子抑制剂，天然产物
Mol文件:	1032350-13-2.mol

MK-2206 2HCl 性质

MK-2206 2HCl 用途与合成方法

生物活性	MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。Phase 2。
体外研究	MK-2206是变构抑制剂，由pleckstrin同源结构域激活。MK-2206抑制Akt的苏氨酸308位点和丝氨酸473位点的自身磷酸化作用。另外，MK-2206阻止Akt调节的下游信号分子（包括TSC2, PRAS40，及核糖体S6蛋白）的磷酸化作用。与抑制Ras 突变型细胞系(如NCI-H358, NCI-H23, NCI-H1299, 和Calu-6)相比，MK-2206 更有效地抑制Ras野生型细胞系(如A431, HCC827, 和NCI-H292)。MK-2206和细胞毒素药剂如erlotinib 和lapatinib联用作用于肺部NCI-H460肿瘤细胞或者卵巢A2780肿瘤细胞，MK-2206也显示出协同效应。
体内研究	MK-2206和这些细胞毒素药剂联用作用于NCI-H292移植瘤，MK-2206显示出非常有效的抗癌活性。卵巢癌A2780移植瘤中，按动物体重，每千克处理240mg MK-2206,则可抑制70%以上的Akt1/2在苏氨酸308位点和丝氨酸473位点的磷酸化，导致肿瘤生长抑制率达到60%。
特征	MK-2206是第一个进入临床研究阶段的Akt小分子变构抑制剂。