现货供应，美国进口， MK-2206 dihydrochloride ，目录号S1078 ，CAS号:1032350-13-2， PI3K / mTOR / AKT ，AKT 抑制剂，Selleck

价格： ￥2079

品牌：Selleck

货号：S1078

产品详情

技术数据:

分子量(MW):	480.39
化学式:	C₂₅H₂₁N₅O.2HCl
溶解度:	DMSO ≥8mg/mL Water ≥20mg/mL Ethanol <1mg/mL
纯度:	99%
稳定性:	at -20℃ 2 years
CAS号:	1032350-13-2

生物活性

MK-2206高度选择性地抑制Akt,作用于Akt1, Akt2和Akt3 时IC50 分别为8, 12 和65 nM。MK-2206是变构抑制剂，由pleckstrin 同源结构域激活。MK-2206抑制Akt的苏氨酸308位点和丝氨酸473位点的自身磷酸化作用。另外，MK-2206阻止Akt调节的下游信号分子（包括TSC2, PRAS40，及核糖体S6蛋白）的磷酸化作用。与抑制Ras 突变型细胞系(如NCI-H358, NCI-H23, NCI-H1299, 和Calu-6)相比，MK-2206 更有效地抑制Ras 野生型细胞系(如A431, HCC827, 和NCI-H292)。MK-2206和细胞毒素药剂如erlotinib 和lapatinib联用作用于肺部NCI-H460肿瘤细胞或者卵巢A2780肿瘤细胞，MK-2206 也显示出协同效应。MK-2206和这些细胞毒素药剂联用作用于NCI-H292移植瘤，MK-2206显示出非常有效的抗癌活性。卵巢癌A2780移植瘤中，按动物体重，每千克处理240mg MK-2206,则可抑制70%以上的Akt1/2在苏氨酸308位点和丝氨酸473位点的磷酸化，导致肿瘤生长抑制率达到60%。^[1] MK-2206用于治疗卵巢癌，原发性腹膜癌，及输卵管肿瘤目前还处于二期临床实验阶段。MK-2206最初是由Merck研究的。

参考文献

[1] Yan L, AACR Annual Meeting 2009: Abstract Number: DDT01-1.
[2] Hirai H, et al, Mol Cancer Therapy, 2010, 9(7), 1956-1967.
[3] http://worldwide.espacenet.com/publicationDetails/biblio?CC=WO&NR=2008070016A2&KC=A2&FT=D&ND=5&date=20080612&DB=EPODOC&locale=en_EP

客户反馈数据

	C.U87MG cells were treated with vehicle or 1 μM MK-2206 for 1 hr, and then irradiated with 6 Gy. Total cell lysate was harvested 1 hr after IR and subjected to Western blot analysis with the indicated antibody. Cells without IR treatment were used as a control. D. Cells were treated with vehicle (control) or 1 μM MK-2206 for 1 hr, then irradiated with indicated dosage. 4 hr after IR, cells were fed with drug-free medium, and incubated for another 20 hr at 37°C, after which they were trypsinized and seeded for clonogenic survival assay. Colony-forming efficiency was determined 14 d later.
	After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of MK-2206 for 3h,followed by 15-minute stimolation of 100ng/ml EGF.
	Effect of selected agents on NOx and cGMP formation induced by AEA. Washed platelets (1.0109 platelets/mL), prewarmed at 378C with saline or 1mM SR1, 1mM SR2, 20 mMURB597 (URB), 1mMMK2206 (MK) or 20 mMLY294002 (LY), were incubated for 1min with 100 mML-arginine in the presence of 1.0 mMAEA. NOx (panel A) and cGMP (panel B) content were determined as detailed in Methods. Each bar represents the meanSD of five independent experiments carried out in triplicate. Student’s t-test: P <0.0001 versus none;P <0.0005; §P <0.005 versus AEA
	Confocal microscopy images of NO formation. DAF 2 DA-loaded washed platelets (1.0109 platelets/mL) were preincubated at 378C with saline (A), and then stimulated for 1min with 0.1 (B), 1.0 (C) or 10 (D) mM AEA. In Panel (E–F–G) washed platelets were preincubated with 1 mM SR1 (E), 1 Mm MK2206 (F) or 20 mM LY294002 (G), and then stimulated for 1min with 1.0 mM AEA. In panel (H) is reported the effect of 5 mg/mL collagen, used as a positive control. All the experiments were carried out in the presence of 100 mM L-arginine. NO formation was visualized by confocal microscropy as detailed in Methods.
	The AEA effect on eNOS phosphorylation. Washed platelets (1.0109 platelets/mL), preincubated at 378C with saline, 1 mM SR1, 1mM SR2, 20 mM LY294002, 1mM MK2206, 1.0mM EGTA, or 30 mM BAPTA/AM, were stimulated for 1 min with 1.0 mM AEA. At the end of incubation suitable aliquots were immunoblotted with anti-p-eNOSser1177 as detailed in Methods.Blots are representative of five independent experiments.
	Mean IL-8 concentrations determined by ELISA of the supernatants of HeLa cells infected with wild-type Salmonella. Kinase inhibitors are indicated on the x axis, and the target families of the inhibitors are indicated above each column. CEC, chelerythrine; Pim Inh, Pim-1 inhibitor 2. Inhibitors that significantly affected IL-8 production relative to the control (P < 0.05, Bonferroni post hoc test from one-way ANOVA) are indicated with an asterisk. Relative cell viability is also shown, as determined by reduction of XTT by viable cells. A450, absorbance at 450 nm.

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