MK-2206 dihydrochloride(Synonyms: MK-2206 (2HCl))

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MK-2206 dihydrochloride (Synonyms: MK-2206 (2HCl)) 纯度: 99.73%

MK-2206 dihydrochloride (MK-2206 (2HCl)) 是一种具有口服活性的，高效选择性的，变构 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 的 IC50 分别为 8、12 和 65 nM。许多乳腺癌细胞系、PIK3CA 突变体和 PTEN 丢失细胞系对 MK-2206 dihydrochloride 敏感。具有抗癌活性。

MK-2206 dihydrochloride(Synonyms: MK-2206 (2HCl))

MK-2206 dihydrochloride Chemical Structure

CAS No. : 1032350-13-2

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥935 In-stock
5 mg ￥850 In-stock
10 mg ￥1172 In-stock
50 mg ￥2900 In-stock
100 mg ￥4100 In-stock
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生物活性

MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy[1][3].

IC50 & Target[1]

Akt1

8 nM (IC50)

Akt2

12 nM (IC50)

Akt3

65 nM (IC50)

体外研究
(In Vitro)

MK-2206 dihydrochloride (MK-2206 (2HCl)) (0-10 μM; 72 and 96 hours) inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner[1].
MK-2206 dihydrochloride (0-10 μM; 24 and 48 hours) results in a dose-dependent increase in the percentage of cells in G0/G1 phase and a concomitant reduction of cell numbers in S phase in CNE-2 and HONE-1 cells[3].
MK-2206 dihydrochloride (0-10 μM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not effect phosphorylation of GSKα/β and AKT[3].
MK-2206 dihydrochloride (0-10 μM; 24 hours) increases the appearance of LC3-II in CNE-2 cells dose-dependently. Microtubule-associated protein 1 LC3 is an essential autophagy protein[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1
Concentration: 0.08, 0.16, 0.31, 0.63, 1.25, 2.5, 5, 10 μM
Incubation Time: 72 and 96 hours
Result: At 72 and 96 hours, the IC50 values in CNE-1, CNE-2, and HONE-1 cell lines were 3-5 μM, and in SUNE-1, they were less than 1 μM.

Cell Cycle Analysis[3]

Cell Line: CNE-2 and HONE-1 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 or 48 hours
Result: Induced cell cycle arrest at G1 in a dose-dependent manner.

Western Blot Analysis[3]

Cell Line: SUNE-1 and CNE-2 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Inhibited phosphorylation of AKT downstream targets.

Cell Autophagy Assay[3]

Cell Line: CNE-2 cells
Concentration: 0.625, 1.25, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Induced autophagy.

体内研究
(In Vivo)

Both MK-2206 dihydrochloride (MK-2206 (2HCl)) doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice[3].
MK-2206 dihydrochloride (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts[3]
Dosage: 240 mg/kg and 480 mg/kg
Administration: Oral gavage; 240 mg/kg for three times a week; 480 mg/kg for once a week; for 2 weeks
Result: Both doses inhibited the growth of human CNE-2 xenografts in nude mice.

Clinical Trial

分子量

480.39

Formula

C25H23Cl2N5O
CAS 号

1032350-13-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 16.67 mg/mL (34.70 mM; ultrasonic and warming and heat to 70°C)

H2O : 3.57 mg/mL (7.43 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 20% SBE-β-CD in saline

    Solubility: 25 mg/mL (52.04 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.48 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.48 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.48 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.48 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Li Yan, et al. Abstract #DDT01-1: MK-2206: A potent oral allosteric AKT inhibitor. 2009.

    [2]. Xing Y, et al. Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/PTEN mutation. Breast Cancer Res. 2019 Jul 5;21(1):78.

    [3]. Zhao YY, et al. Effects of an oral allosteric AKT inhibitor (MK-2206) on human nasopharyngeal cancer in vitro and in vivo. Drug Des Devel Ther. 2014 Oct 10;8:1827-37.

    [4]. Agarwal E, et al. Akt inhibitor MK-2206 promotes anti-tumor activity and cell death by modulation of AIF and Ezrin in colorectal cancer. BMC Cancer. 2014 Mar 1;14:145.

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