AKT inhibitor VIII |
| Catalog No.GC11589 |
A potent inhibitor of Akt1 and Akt2
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 612847-09-3
Sample solution is provided at 25 µL, 10mM.
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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.
| 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. |
|
Reacting condition |
10-100 μM for 24, 48, and 72 h |
|
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 |
|
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. |
|
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. |
|
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. | |
| Cas No. | 612847-09-3 | SDF | |
| Chemical Name | 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 | ||
| Formula | C34H29N7O | M.Wt | 551.64 |
| Solubility | ≥ 9.2 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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