MK-2206 dihydrochloride
Catalog No.
A3010
Akt1/2/3抑制剂
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MK-2206 dihydrochloride是一种选择性的Akt1/2/3抑制剂。MK-2206抑制Akt Thr308和Ser 473的磷酸化。作为单一药剂或与其它化疗剂结合使用，MK-2206均可以抑制Akt信号通路并促进癌细胞死亡。MK-2206通过活性氧可以增加rapamycin的敏感性。MK-2206与etoposide或rapamycin联合使用可以显著增加抗肿瘤效应。
参考文献：
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2. First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors. TA Yap, L Yan, A Patnaik, I Fearen. Journal of Clinical Oncology 2011
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 480.39 |
| Cas No. | 1032350-13-2 |
| Formula | C25H21N5O·2HCl |
| Synonyms | MK-2206, MK2206, MK 2206 |
| Solubility | insoluble in EtOH; ≥12.01 mg/mL in DMSO; ≥2.74 mg/mL in H2O with ultrasonic |
| Chemical Name | 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one;dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
异位内膜间质细胞 |
|
溶解方法 |
在DMSO中的溶解度 >10 mM。为了获得更高的浓度，可以将离心管在37°C加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20°C以下储存几个月。 |
|
反应时间 |
100 nM，2 h |
|
应用 |
从无疾病复发患者中分离的异位内膜间质细胞（OSIS）而非在位内膜间质细胞中，在缺乏R5020时，用MK-2206抑制AKT或U0126抑制MEK1/2, 24小时后可以增加总的和核内PRA和PRB蛋白的水平。MK-2206和R5020减少OSIS的活力，增加细胞凋亡。MK-2206和孕激素也可以减少SC移植子宫内膜异位症组织的体积。 |
| 动物实验[1]： | |
|
动物模型 |
5 周龄CD-1裸鼠 |
|
剂量 |
360 mg/kg/d，15天；口服灌胃。 |
|
应用 |
MK-2206与孕激素（progesterone）之间无显著的相互作用（P=0.628）。MK-2206（P=0.077）和孕激素（P=0.087）都可以减少肿瘤体积。MK-2206可以减少Ki67的水平。在E2（E）和E+progesterone（P）治疗组，裂解的caspase-3 (CC3)的水平是非常低的，而MK-2206增加CC3的水平，尤其是在P存在时。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: 1. Eaton JL1, Unno K, Caraveo M et al. Increased AKT or MEK1/2 activity influences progesterone receptor levels and localization in endometriosis. J Clin Endocrinol Metab. 2013 Dec;98(12):E1871-9. |
|
| 描述 | MK-2206 2HCl是一种选择性的Akt1/2/3抑制剂，IC50值分别为8 nM/12 nM/65 nM。 | |||||
| 靶点 | Akt1 | Akt2 | Akt3 | |||
| IC50 | 8 nM | 12 nM | 65 nM | |||
质量控制和MSDS
- 批次:
化学结构
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