MK-2206

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MK-2206

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。

CAS NO:

1032349-77-1

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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。

生物活性

MK-2206 is an orally active, highly potent and selective allostericAktinhibitor, withIC₅₀s of 8, 12, and 65 nM forAkt1,Akt2, andAkt3, respectively. Many breastcancercell lines, and PIK3CA-mutant and cell lines withPTENloss are sensitive to MK-2206. Anticancer activities^[1]^[2].

IC₅₀& Target^[1]

Akt1

8 nM ()

Akt2

12 nM ()

Akt3

65 nM ()

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].

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 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].

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

443.93

Formula

C₂₅H₂₂ClN₅O

CAS 号

1032349-77-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.