FPA 124
(Synonyms: AKT抗化剂,Akt Inhibitor XI) 目录号 : GC17984A cell-permeable Akt inhibitor
Cas No.:902779-59-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
The kinase Akt (also known as protein kinase B or PKB) modulates cell proliferation, metabolism, and survival, as well as angiogenesis.[1],[2] Akt inhibitor XI is a cell-permeable, copper-containing 3-formylchromone derivative that inhibits Akt in an array of cancer cells (IC50s = 10-34 µM).[3] It also causes NF-κB inactivation in an orthotopic pancreatic tumor model using COLO 357 cells.3 Molecular modeling indicates that this inhibitor interacts with the pleckstrin homology and kinase domains of Akt. Akt inhibitor XI is commonly used in the range of 1-20 µM to assess the role of Akt in cellular responses.[4],[5],[6]
Reference:
[1]. Manning, B.D., and Cantley, L.C. AKT/PKB signaling: Navigating downstream. Cell 129(7), 1261-1274 (2007).
[2]. Yuan, T.L., and Cantley, L.C. PI3K pathway alterations in cancer: Variations on a theme. Oncogene 27(41), 5497-5510 (2008).
[3]. Barve, V., Ahmed, F., Adsule, S., et al. Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells. Journal of Medicinal Chemistry 49(13), 3800-3808 (2006).
[4]. Frampton, G., Invernizzi, P., Bernuzzi, F., et al. Interleukin-6-driven progranulin expression increases cholangiocarcinoma growth by an Akt-dependent mechanism. Gut 61(2), 268-277 (2012).
[5]. Rybchyn, M.S., Slater, M., Conlgrave, A.D., et al. An Akt-dependent increase in canonical Wnt signaling and a decrease in sclerostin protein levels are involved in strontium ranelate-induced osteogenic effects in human osteoblasts. The Journal of Biological Chemisty 286(27), 23771-23779 (2011).
[6]. Zareen, N., Biswas, S.C., and Greene, L.A. A feed-forward loop involving Trib3, Akt and FoxO mediates death of NGF-deprived neurons. Cell Death and Differentiation 20(12), 1719-1730 (2013).
| Cas No. | 902779-59-3 | SDF | |
| 别名 | AKT抗化剂,Akt Inhibitor XI | ||
| 化学名 | copper(II) (Z)-2-((4-oxo-4H-chromen-3-yl)methylene)hydrazinecarbimidothioate chloride hydrochloride | ||
| Canonical SMILES | N=C([S-])N/N=C([H])\C1=COC2=CC=CC=C2C1=O.[Cl-].Cl.[Cu+2] | ||
| 分子式 | C11H9Cl2CuN3O2S | 分子量 | 381.73 |
| 溶解度 | DMSO: 0.1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6197 mL | 13.0983 mL | 26.1965 mL |
| 5 mM | 0.5239 mL | 2.6197 mL | 5.2393 mL |
| 10 mM | 0.262 mL | 1.3098 mL | 2.6197 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。