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MK-2206 dihydrochloride

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产品编号 T1952Cas号 1032350-13-2
别名 MK-2206 2HCl

MK-2206 dihydrochloride (MK-2206 2HCl) 是一种变构 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3 (IC50=8/12/65 nM),具有口服活性的、高效选择性。MK-2206 dihydrochloride 具有抗肿瘤活性。

MK-2206 dihydrochloride

MK-2206 dihydrochloride

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纯度: 99.91%
产品编号 T1952 别名 MK-2206 2HClCas号 1032350-13-2

MK-2206 dihydrochloride (MK-2206 2HCl) 是一种变构 Akt 抑制剂,抑制 Akt1、Akt2 和 Akt3 (IC50=8/12/65 nM),具有口服活性的、高效选择性。MK-2206 dihydrochloride 具有抗肿瘤活性。

规格价格库存数量
1 mg¥ 298现货
2 mg¥ 428现货
5 mg¥ 689现货
10 mg¥ 969现货
25 mg¥ 1,620现货
50 mg¥ 2,380现货
100 mg¥ 3,380现货
200 mg¥ 4,830现货
500 mg¥ 7,380现货
1 mL x 10 mM (in DMSO)¥ 773现货
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产品介绍

生物活性
产品描述
MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.
靶点活性
Akt3:65 nM (cell free), Akt2:12 nM (cell free), Akt1:8 nM (cell free)
体外活性
方法:14 种肿瘤细胞用 MK-2206 dihydrochloride 处理 72 h,使用 CellTiter-Glo assay 检测细胞活力。
结果:MK-2206 dihydrochloride 抑制肿瘤细胞生长,IC50 在 0.1-28.6 μmol/L之间。[1]
方法:人鼻咽癌细胞系 CNE-2、HONE-1 用 MK-2206 dihydrochloride (0.625-10 μM) 处理 24-48 h,使用 Flow Cytometry 方法检测细胞周期情况。
结果:MK-2206 dihydrochloride 导致 G0/G1 期细胞百分比的剂量依赖性增加和 S 期细胞数量的减少。MK-2206 dihydrochloride 诱导细胞周期停滞于 G1 期。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 MK-2206 dihydrochloride (120 mg/kg 每周三次或 360 mg/kg 每周一次,30% Captisol) 和 erlotinib (50 mg/kg 每周五次,0.5% methylcellulose + 0.1% Tween 80) 口服给药给携带人肺癌肿瘤 NCI-H292 的 CD1 小鼠,持续两周。
结果:每周三次的 MK-2206 单药治疗无效,每周一次的方案仅介导中等的抗肿瘤疗效。尽管 erlotinib 单独介导了显著的肿瘤生长抑制,但与 MK-2206 的联合治疗显著增强了其抗肿瘤疗效,包括肿瘤消退。[1]
方法:为检测体内抗肿瘤活性,将 MK-2206 dihydrochloride (120 mg/kg in 30% captisol) 灌胃给药给携带人子宫内膜癌肿瘤的 NSG 小鼠,每周两次,持续三周。
结果:MK-2206 dihydrochloride 治疗使 3 种不同类型和等级的 PDX 肿瘤的生长都受到显著抑制。[3]
细胞实验
Cells were seeded at a density of 2 to 3 × 103 per well in 96-well plates. Twenty-four hours after plating, varying concentrations of the drug, either as a single agent or in combination, were added to the wells. Cell proliferation was determined by using the CellTiter-Glo assay at 72 or 96 hours after dosing. The nature of the drug interaction was evaluated by using the combination index (CI) according to the method of Chou and Talalay. A commercial software package was obtained from Calcusyn. In combination with docetaxel, we tested three treatment sequences: (a) MK-2206 followed by docetaxel—cells were exposed to MK-2206 for 24 hours, and then after washout of MK-2206, cells were treated with docetaxel for an additional 72 hours; (b) docetaxel followed by MK-2206—cells were exposed to docetaxel for 24 hours, and then after washout of docetaxel, cells were treated with MK-2206 for an additional 72 hours; and (c) concurrent treatment—cells were exposed to both MK-2206 and docetaxel for 72 hours [2].
动物实验
When the mean tumor size reached 0.13 cm3 for the SK-OV-3 or 0.2 cm3 for the NCI-H292, HCC70, PC-3, and NCI-H460 models, the mice were randomized into control and treatment groups with approximately equivalent ranges of tumor volume between groups (n = 5 animals per group). The following vehicles were used to dose the compounds: 30% Captisol (Cydex) for MK-2206; 0.5% methylcellulose + 0.1% Tween 80 for erlotinib; distilled water for lapatinib; 0.73% ethanol in saline for docetaxel; and saline for carboplatin and gemcitabine. The control group received vehicle only. Tumor volume was measured with calipers twice a week. Animal body weight and physical signs were monitored during the experiments. Tumor volume was calculated, taking length to be the longest diameter across the tumor and width to be the perpendicular diameter, by using the following formula: (length × width)2 × 0.5. Relative tumor volume was assessed by dividing the tumor volume on different observation days with the starting tumor volume. Statistical significance was evaluated by using the two-way repeated ANOVA test followed by Dunnett's test or an unpaired t-test [2].
别名MK-2206 2HCl
化学信息
分子量480.39
分子式C25H23Cl2N5O
CAS No.1032350-13-2
SmilesCl.Cl.NC1(CCC1)c1ccc(cc1)-c1nc2ccn3c(n[nH]c3=O)c2cc1-c1ccccc1
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 7.5 mg/mL (15.61 mM)
10% DMSO+90% Saline: 0.75 mg/mL (1.56 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
10% DMSO+90% Saline/DMSO
1mg5mg10mg50mg
1 mM2.0816 mL10.4082 mL20.8164 mL104.0821 mL
DMSO
1mg5mg10mg50mg
5 mM0.4163 mL2.0816 mL4.1633 mL20.8164 mL
10 mM0.2082 mL1.0408 mL2.0816 mL10.4082 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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