AKT inhibitor VIII
(Synonyms: 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,AKTi-1/2) 目录号 : GC11589
A potent inhibitor of Akt1 and Akt2
Cas No.:612847-09-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
MCF-7 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >9.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10-100 μM for 24, 48, and 72 h |
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Applications |
AKT inhibitor VIII significantly inhibited the proliferation and increased the LDH release in both cell lines in a dose-dependent manner. AKT inhibitor VIII dose-dependently induced cell cycle arrest at the G0/G1 phase. The protein expressions of p-cyclin D1, total cyclin D1, p-CDK2, total CDK2, pRb, total Rb, Bcl-xL, and Akt were significantly inhibited by AKT inhibitor VIII, whereas the protein expressions of Bad and Bax, and the proteolytic cleavage of caspase-9, caspase-7, and polyADP-ribose polymerase (PARP) were dramatically increased. |
| Animal experiment [1]: | |
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Animal models |
BALB/c nude mice |
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Dosage form |
15 mg/kg and 30 mg/kg by intraperitoneal administration once daily for 8 days |
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Application |
AKT inhibitor VIII dose-dependently suppressed the tumor growth in vivo, achieving 32% and 54% inhibition rates after intraperitoneal injection of 15 mg/kg and 30 mg/kg, respectively. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] [1] Zhong Z, Dang Y, Yuan X, Guo W, Li Y, Tan W, Cui J, Lu J, Zhang Q, Chen X, Wang Y. Furanodiene, a natural product, inhibits breast cancer growth both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90. | |
AKT inhibitor VIII is a cell-permeable, reversible and potent, selective inhibitor of Akt1, Akt2 and Akt3 with IC50 values of 58 nM, 210 nM and 2.12 μM, respectively.
AKT inhibitor VIII has shown to remarkably increase anti-proliferation induced by furanodiene in human breast cancer cell MCF-7. AKT inhibitor VIII could enhance the furanodiene- stimulated Akt and p-Akt expression decreases as well as increase furanodiene-induced PARP cleavage in MCF-7 cells [1].
AKT inhibitor VIII has been revealed to inhibit IGF-1-induced Akt phosphorylation in a concentration-dependent manner. AKT inhibitor VIII has also been demonstrated to reduce PRAS40 phosphorylation in PC12 cells [2].
Reference:
[1] Zhong Z1, Dang Y, Yuan X, Guo W, Li Y, Tan W, Cui J, Lu J, Zhang Q, Chen X, Wang Y. Furanodiene, a natural product, inhibits breast cancer growth both in vitro and in vivo. Cell Physiol Biochem. 2012;30(3):778-90.
[2] Wang H1, Zhang Q, Zhang L, Little PJ, Xie X, Meng Q, Ren Y, Zhou L, Gao G, Quirion R, Zheng W. Insulin-like growth factor-1 induces the phosphorylation of PRAS40 via the PI3K/Akt signaling pathway in PC12 cells. Neurosci Lett. 2012 May 10;516(1):105-9.
| Cas No. | 612847-09-3 | SDF | |
| 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,AKTi-1/2 | ||
| 化学名 | 3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one | ||
| Canonical SMILES | C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=NC6=CC7=C(C=C6N=C5C8=CC=CC=C8)N=CN7 | ||
| 分子式 | C34H29N7O | 分子量 | 551.64 |
| 溶解度 | ≥ 9.2 mg/mL in DMSO | 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。 |
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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 | 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 |
| 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。