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抑制剂/激活剂

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凋亡与自噬

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MK-2206 dihydrochloride

MK-2206 dihydrochloride MK-2206 (2HCl)

MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，在无细胞试验中IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。MK-2206 2HCl 在肿瘤细胞中可诱导自噬和凋亡。Phase 2。

货号：
TK0154
规格：

1mg

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1032350-13-2
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.
分子式	C25H21N5O
分子量	480.39
储存条件	Powder -20℃ 3 years
溶解性数据	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)
体内研究	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. 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.
体外研究	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. 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. 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. 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.
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纯度及产品资料	98%

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