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MK-2206
MK-2206 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 中的 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 敏感。具有抗癌活性。
MK-2206 Chemical Structure
CAS No. : 1032349-77-1
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
MK-2206 的其他形式现货产品:
MK-2206 dihydrochloride
| 生物活性 |
MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities[1][2].
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| IC50 & Target[1] |
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Akt1
8 nM ()
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Akt2
12 nM ()
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Akt3
65 nM ()
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体外研究
(In Vitro) |
MK-2206 (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[3].
MK-2206 (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 (0-10 μM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not affect phosphorylation of GSKα/β and AKT[3].
MK-2206 (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].
Shanghai Jinpan Biotech Co Ltd 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. |
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体内研究
(In Vivo) |
Both MK-2206 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 (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].
Shanghai Jinpan Biotech Co Ltd 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. |
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| Clinical Trial |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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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