MK-2206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。
别名:MK-2206 dihydrochloride
MK-2206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。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。
细胞实验 | |
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细胞系 | CNE-1,CNE-2,HONE-1,SUNE-1 |
方法 | MK-2206 is dissolved in DMSO as a stock solution and diluted by culture media before use. Cells are seeded at an appropriate density per well in 96-well plates and incubated for 24 hours. Then MK-2206 (0~10μM) is added to the cells. Cell proliferation is determined after 72 or 96 hours. |
浓度 | 0,0.08,0.16,0.31,0.63,1.25,2.5,5,10μM |
处理时间 | 72 or 96 hours |
动物实验 | |
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动物模型 | CNE-2 model in male BALB/c nude mice |
配制 | Formulated in 30% Captisol |
剂量 | MK-2206 (240 mg/kg, three times a week), MK-2206 (480 mg/kg, once a week), and 30% Captisol (Cydex) diluents |
给药处理 | Oral gavage for 2 weeks |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
分子量 | 480.39 |
分子式 | C25H21N5O.2HCl |
CAS号 | 1032350-13-2 |
纯度 | 100.00% |
溶解性(25°C) | 12mg/mL in DMSO |
储存和运输条件 |
固体粉末: -20°C 冷藏长期储存
常温运输及临时存放 |
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.0816 mL | 10.4082 mL | 20.8164 mL |
5 mM | 0.4163 mL | 2.0816 mL | 4.1633 mL |
10 mM | 0.2082 mL | 1.0408 mL | 2.0816 mL |
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Overexpression of ribonuclease inhibitor induces autophagy in human colorectal cancer cells via the Akt/mTOR/ULK1 pathway.
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Inhibition of AKT suppresses the initiation and progression of BRCA1-associated mammary tumors.
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Tight Junction Proteins Claudin-1 and Occludin Are Important for Cutaneous Wound Healing
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Oncotarget. 2016 Feb 22.
Mechanosensitive caveolin-1 activation-induced PI3K/Akt/mTOR signaling pathway promotes breast cancer motility, invadopodia formation and metastasis in vivo.
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Cell Signal. 2015 Nov;2191-200.
Discontinuing MEK inhibitors in tumor cells with an acquired resistance increases migration and invasion.
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J Cancer. 2015 Sep 16;1195-205.
Vertical Targeting of AKT and mTOR as Well as Dual Targeting of AKT and MEK Signaling Is Synergistic in Hepatocellular Carcinoma.
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Biochem Pharmacol. 2015 Aug 15;323-36.
Arctigenin exerts anti-colitis efficacy through inhibiting the differentiation of Th1 and Th17 cells via an mTORC1-dependent pathway.
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Invest New Drugs. 2014 Dec;32(6):1144-54.
Dual Inhibition of PI3K-AKT-mTOR- and RAF-MEK-ERK-signaling is synergistic in cholangiocarcinoma and reverses acquired resistance to MEK-inhibitors.
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Int J Cancer. 2013 Nov;133(9):2065-76.
Combined targeting of AKT and mTOR using MK-2206 and RAD001 is synergistic in the treatment of cholangiocarcinoma.
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Phosphatidylinositol 3-Kinase/Akt Signaling Pathway Activates the WNK-OSR1/SPAK-NCC Phosphorylation Cascade in Hyperinsulinemic db/db Mice.
Nishida et al. Hypertension. 2012 Sep 4. PMID: 22949526.
Biomarkers of Response to Akt Inhibitor MK-2206 in Breast Cancer.
Sangai et al. Clin Cancer Res. 2012 Aug 29. PMID: 22932669.
Inhibition of AKT with the Orally Active Allosteric AKT Inhibitor, MK-2206, Sensitizes Endometrial Cancer Cells to Progestin.
Pant et al. PLoS One. 2012;7(7):e41593. PMID: 22911820.
Harnessing the PI3K/Akt/mTOR pathway in T-cell acute lymphoblastic leukemia: Eliminating activity by targeting at different levels.
Bressanin et al. Oncotarget. 2012 Aug 9. PMID: 22885370.
A novel PKB/Akt inhibitor, MK-2206, effectively inhibits insulin-stimulated glucose metabolism and protein synthesis in isolated rat skeletal muscle.
Lai et al. Biochem J. 2012 Jul 13. PMID: 22793019.
Cytotoxic activity of the novel Akt inhibitor, MK-2206, in T-cell acute lymphoblastic leukemia.
Simioni et al. Leukemia. 2012 May 22. PMID: 22614243.
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