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MK-2206 dihydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MK-2206 dihydrochloride图片
CAS NO:1032350-13-2
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
MK-2206 (2HCl)
产品介绍
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。
生物活性

MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active allostericAKTinhibitor withIC50s of 5 nM, 12 nM, and 65 nM forAKT1,AKT2, andAKT3, respectively. MK-2206 dihydrochloride inducesautophagy[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].

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 IC50values 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].

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

性状

Solid

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℃)

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0816 mL10.4082 mL20.8164 mL
5 mM0.4163 mL2.0816 mL4.1633 mL
10 mM0.2082 mL1.0408 mL2.0816 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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-CDin 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 μL20% 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本网站选购。