产品
编 号：F014483
分子式：C25H22ClN5O
分子量：443.93
分子式：C25H22ClN5O
分子量：443.93
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CAS No: 1032349-77-1
产品详情
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. MK-2206 has anticancer activities.
体内研究：
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.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.Animal Model:Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts
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.
体外研究：
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.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.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.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.
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. MK-2206 has anticancer activities.
体内研究：
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.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.Animal Model:Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts
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.
体外研究：
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.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.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.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.
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