AKT inhibitor VIII|612847-09-3|(AKTi-1/2)-陌孚医药/Medlife

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AKT inhibitor VIII (Synonyms: AKTi-1/2)

目录号: PC15427 纯度: ≥98%

CAS No. :612847-09-3

商品编号	规格	价格	会员价
PC15427-10mg	10mg	¥1421.00	请登录
PC15427-25mg	25mg	¥3430.00	请登录
PC15427-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1274.00	请登录

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中文名称

AKT inhibitor VIII

中文别名

1,3-二氢-1-[1-[[4-(6-苯基-1H-咪唑并[4,5-G]喹喔啉-7-基)苯基]甲基]-4-哌啶基]-2H-苯并咪唑-2-酮;1-(1-(4-(6-苯基-1H-咪唑并[4,5-g]喹噁啉-7-基)苄基)哌啶-4-基)-1H-苯并[d]咪唑-2(3H)-酮;AKT抑制剂VIII;AKT inhibitor VIII 抑制剂;1,3-二氢-1-[1-[4-(6-苯基-1H-咪唑并[4,5-g]喹喔啉-7-基)苯基甲基]-4-哌啶基]-2H-苯并咪唑-2-酮

英文名称

AKT inhibitor VIII

英文别名

1-(1-(4-(6-Phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one;AKT inhibitor VIII;1-(1-(4-(6-Phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)benzyl)-piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one;2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]...;2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-;3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one;1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one;Akt Inhibitor VIII, Isozyme-Selective, Akti-1;AKTI-1;imidazoquinoxaline 16h;1,3-Dihydro-1-[1-[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenylmethyl]-4-piperidinyl]-2H-benzimidazol-2-one;1,3-Dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-2H-benzimidazol-2-one;Akti-1/2;Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2;InSolution™ Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2;1-{1-

Cas No.

612847-09-3

分子式

C₃₄H₂₉N₇O

分子量

551.64

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC₅₀s of 58 nM, 210 nM, and 2119 nM, respectively.

性状

Solid

IC50 & Target[1][2]

Akt1

58 nM (IC₅₀)

Akt2

210 nM (IC₅₀)

Akt3

2119 nM (IC₅₀)

体外研究(In Vitro)

When LnCaP cells are pretreated with AKT inhibitor VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT inhibitor VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by Akt inhibitor VIII pretreatment. The Akt inhibitor VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions. AKT inhibitor VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Mice are dosed with AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Lindsley, et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg. Med. Chem. Lett. (2005), 15(3), 761-764. [Information]

[2]. Zhong Z, et al. Furanodiene, a Natural Product, Inhibits Breast Cancer Growth Both 体外研究 and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. Epub 2012 Aug 2. [Information]

[3]. Leonardo Romorini, et al. AKT/GSK3β signaling pathway is critically involved in human pluripotent stem cell survival. Sci Rep. 2016; 6: 35660

溶解度数据

体外研究:

DMSO : 20 mg/mL (36.26 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8128 mL	9.0639 mL	18.1278 mL
5 mM	0.3626 mL	1.8128 mL	3.6256 mL
10 mM	0.1813 mL	0.9064 mL	1.8128 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2 mg/mL (3.63 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (3.63 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (3.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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