MK-2206 2HCl, AKT 丝氨酸/苏氨酸激酶 1 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 2 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 3 的变构调节剂

MK-2206 2HCl

M408752-1ml

1ml

Moligand™

10mM in DMSO

-80℃储存

超低温冰袋运输

MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，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。A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain Information In vitro MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells. MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death. In vivo MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg. MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib. Cell Data cell lines： tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT) Concentrations： 0, 0.3, 1 and 3 μM Incubation Time： 72 or 96 hours Powder Purity:≥99%

MK-2206 2HCl 是一种高选择性的 Akt1/2/3 抑制剂，在无细胞实验中的 IC50 分别为 8 nM/12 nM/65 nM；未观察到对其他 250 种蛋白激酶的抑制活性。MK-2206 2HCl 可诱导癌细胞自噬和凋亡。第 2 阶段。

1032350-13-2(DMSO)

C25H21N5O·2HCl

480.39 g/mol

Cl.Cl.NC1(CCC1)C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C(=O)NN=C45)C6=CC=CC=C6

Solubility (25°C) In vitro Water: 3 mg/mL (10.74 mM); DMSO: Insoluble; Ethanol: Insoluble;

变构调节剂

AKT 丝氨酸/苏氨酸激酶 1 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 2 的变构调节剂；AKT 丝氨酸/苏氨酸激酶 3 的变构调节剂