China (Mainland)
Premiumsupplier 
MK-2206 2HCl CAS NO.1032350-13-2
- FOB Price: USD: 1.00-1.00 /Gram Get Latest Price
- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
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
- ProName: MK-2206 2HCl
- CasNo: 1032350-13-2
- Molecular Formula: C25H21N5O
- Appearance: White crystal
- Application: CAS：1032350-13-2；MK-2206;8-[4-(1-Amino...
- DeliveryTime: 3 months
- PackAge: 100g,500g,1kg,25kg
- Port: shang hai
- ProductionCapacity: 1000 Metric Ton/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are specialized in custom synthesis, chemical/pharmaceutical/ pesticides outsourcing and contract research.
We are committed to provide excellence in researching, manufacturing and drug discovery process.
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
| 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。 |