α-mangostin
(Synonyms: NSC 27593, NSC 139154) 目录号 : GN10468
PI3K/AKT inhibitor
Cas No.:6147-11-1
Sample solution is provided at 25 µL, 10mM.
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α-mangostin is an inhibitor of PI3K/AKT with IC50 value of 32 μM (pancreatic cancer cell hTERT-HPNE for 48 hours) [1].
PI3K (phosphatidylinositol-3 kinases) is a member of lipid kinase family and has serine / threonine (Ser/Thr) kinase activity. Akt plays an important role in modulating the function of numerous substrates involved in the regulation of cell survival, cell cycle progression and cellular growth. Recently, it has been shown that PI3K/Akt signaling pathway components are frequently oveexpressed in a variety of human cancers [1] [2].
α-mangostin is a potent FAS inhibitor. When pancreatic cancer cell line BxPc-3, α-mangostin treatment suppressed the cell viability and EMT process via suppressing the activation of PI3K/AKT pathway[1].
In BALb/c nude mice model with BxPc-3 cells xenograft, administration ofα-mangostin (50 or 100 mg.kg) dramatically inhibited tumor growth with a dose-dependent manner [1].
It is also reported thatα-mangostin could target other signaling pathway. In breast cancer cell line, α-mangostin suppressed FAS expression and inhibited intracellular FAS activity that resulted in the cells apoptosis [3]. When tested with breast cancer cell line MCF-7, α-mangostin promoted cell apoptosis via regulating NF-κB, Bax/Bcl-2 and heat shock protein 70 [4].
References:
[1]. Xu, Q., et al., alpha-Mangostin suppresses the viability and epithelial-mesenchymal transition of pancreatic cancer cells by downregulating the PI3K/Akt pathway. Biomed Res Int, 2014. 2014: p. 546353.
[2]. Carnero, A. and J.M. Paramio, The PTEN/PI3K/AKT Pathway in vivo, Cancer Mouse Models. Front Oncol, 2014. 4: p. 252.
[3]. Li, P., W. Tian, and X. Ma, Alpha-mangostin inhibits intracellular fatty acid synthase and induces apoptosis in breast cancer cells. Mol Cancer, 2014. 13: p. 138.
[4]. Ibrahim, M.Y., et al., alpha-Mangostin from Cratoxylum arborescens demonstrates apoptogenesis in MCF-7 with regulation of NF-kappaB and Hsp70 protein modulation in vitro, and tumor reduction in vivo. Drug Des Devel Ther, 2014. 8: p. 1629-47.
Cell experiment: | IDH1+/+ and IDH1 |
Animal experiment: | Rats: Male Wistar rats are divided into 3 groups and treated with intraperitoneal injections of TAA (200 mg/kg). One subgroup is left untreated whereas the other two are treated either with 100 mg/kg alpha-mangostin or vehicle alone (80% DMSO, 20% water), which are administered intraperitoneally 3 times per weekfor a total of4 weeks. The incidence offibrotic nodules on the liver and the serum levels of the liver enzymes aspartate transaminase (AST) and alanine transaminase (ALT) are measured[4]. |
References: [1]. Kim HJ, et al. Discovery of α-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1. Bioorg Med Chem Lett. 2015 Dec 1;25(23):5625-31. | |
| Cas No. | 6147-11-1 | SDF | |
| 别名 | NSC 27593, NSC 139154 | ||
| 化学名 | 1,3,6-trihydroxy-7-methoxy-2,8-bis(3-methylbut-2-enyl)xanthen-9-one | ||
| Canonical SMILES | CC(=CCC1=C(C=C2C(=C1O)C(=O)C3=C(C(=C(C=C3O2)O)OC)CC=C(C)C)O)C | ||
| 分子式 | C24H26O6 | 分子量 | 410.4 |
| 溶解度 | ≥ 135.6mg/mL in DMSO | 储存条件 | |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4366 mL | 12.1832 mL | 24.3665 mL |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8733 mL |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet