3CAI
Based on 4 publication(s) in Google Scholar
3CAI is a potent and specific AKT1 and AKT2 inhibitor.
For research use only. We do not sell to patients.
- Purity: 98.32%
- CAS No.: 28755-03-5
- Formula: C10H8ClNO
- Molecular Weight:193.63
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 3CAI
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Biological Activity
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Akt1 |
Akt2 |
3CAI is a potential inhibitor of AKT. Based on these screening data, the effect of 3CAI on the kinase activities of AKT1, MEK1, JNK1, ERK1 and TOPK is tested using in vitro kinase assays. The results show that 3CAI (1 μM) suppresses only AKT1 kinase activity and the other kinases tested are not affected by 3CAI. 3CAI is a much more potent AKT1 inhibitor than PI3K (60% inhibition at 1 vs 10 μM, respectively). 3CAI substantially suppresses AKT1 activity as well as AKT2 activity in a dose dependent manner. 3CAI inhibits down-stream targets of AKT and induces apoptosis. AKT-mediated phosphorlyation site of mTOR (Ser2448) and GSK3β (Ser9) are substantially decreased by 3CAI in a time-dependent manner. Furthermore, pro-apoptotic marker proteins p53 and p21 are also upregulated by 3CAI after 12 or 24 h of treatment. HCT116 and HT29 colon cancer cells are seeded on 6 cm dishes in 1% FBS/McCoy's 5A (HCT116) with 3CAI (4 μM), I3C or the AKT inhibitor and then incubated for 4 days. Results show that the number of apoptotic cells is significantly increased by 3CAI in HCT116 and HT29 colon cancer cells compared with untreated control cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 28755-03-5
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Appearance Solid
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Molecular Weight 193.63
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Formula C10H8ClNO
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Color Off-white to pink
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SMILES
O=C(CCl)C1=CNC2=CC=CC=C12
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Autophagy
Impaired degradation of PLCG1 by chaperone-mediated autophagy promotes cellular senescence and intervertebral disc degeneration. [Abstract]2025 Feb;21(2):352-373. PMID: 39212196 -
Chin Med J (Engl)
Cell softness reveals tumorigenic potential via ITGB8/AKT/glycolysis signaling in a mice model of orthotopic bladder cancer. [Abstract]2024 Jan 20;137(2):209-221. PMID: 37390491 -
Int J Mol Sci
Leucine Zipper Downregulated in Cancer-1 Interacts with Clathrin Adaptors to Control Epidermal Growth Factor Receptor (EGFR) Internalization and Gefitinib Response in EGFR-Mutated Non-Small Cell Lung Cancer. [Abstract]2024 Jan 23;25(3):1374. PMID: 38338651 -
Solvent & Solubility
DMSO : 250 mg/mL (1291.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (10.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The kinase assay is performed. Briefly, the reaction is carried out in the presence of 10 μCi of [γ-32P]ATP with each compound (e.g., 3CAI, 0.5, 1, 2 and 4 μM) in 40 μL of reaction buffer containing 20 mM HEPES (pH 7.4), 10 mM MgCl2, 10 mM MnCl2, and 1 mM dithiothreitol. After incubation at room temperature for 30 min, the reaction is stopped by adding 10 μL protein loading buffer and the mixture is separated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). The relative amounts of incorporated radioactivity are assessed by autoradiography[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HCT116 or HCT29 colon cancer cells are plated into 60-mm culture dishes (1×105 cells/dish) and incubated for 1 day in medium containing 10% FBS. The culture medium is then replaced with a 1% serum medium and cultured for 4 days with 3CAI (4 μM), I3C or a commercial AKT inhibitor. The cells are collected by trypsinization and washed with phosphate buffered saline (PBS). The cells are resuspended in 200 μL of binding buffer. Annexin V staining is accomplished. The cells are observed under a fluorescence microscope using a dual filter set for FITC and propidium iodide and then analyzed by flow cytometry[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Athymic mice [Cr:NIH(S), NIH Swiss nude, 6-9 wk old] are divided into five groups: 1) untreated vehicle group (n=15); 2) 20 mg 3CAI/kg of body weight (n=15), 3) 30 mg 3CAI/kg body weight (n=15); 4) 100 mg I3C/kg of body weight (n=15); 5) no cells and 30 mg 3CAI/kg of body weight (n=15). HCT116 cells (3×106 cells/100 μL) are suspended in serum free McCoy's 5A medium and inoculated subcutaneously into the right flank of each mouse. 3CAI, I3C or vehicle is administered orally 5 times per week for 21 days. Tumor volume is calculated. Mice are monitored until tumors reach 1 cm3 total volume, at which time mice are euthanized and tumors are extracted.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.1645 mL | 25.8224 mL | 51.6449 mL | 129.1122 mL |
| 5 mM | 1.0329 mL | 5.1645 mL | 10.3290 mL | 25.8224 mL | |
| 10 mM | 0.5164 mL | 2.5822 mL | 5.1645 mL | 12.9112 mL | |
| 15 mM | 0.3443 mL | 1.7215 mL | 3.4430 mL | 8.6075 mL | |
| 20 mM | 0.2582 mL | 1.2911 mL | 2.5822 mL | 6.4556 mL | |
| 25 mM | 0.2066 mL | 1.0329 mL | 2.0658 mL | 5.1645 mL | |
| 30 mM | 0.1721 mL | 0.8607 mL | 1.7215 mL | 4.3037 mL | |
| 40 mM | 0.1291 mL | 0.6456 mL | 1.2911 mL | 3.2278 mL | |
| 50 mM | 0.1033 mL | 0.5164 mL | 1.0329 mL | 2.5822 mL | |
| 60 mM | 0.0861 mL | 0.4304 mL | 0.8607 mL | 2.1519 mL | |
| 80 mM | 0.0646 mL | 0.3228 mL | 0.6456 mL | 1.6139 mL | |
| 100 mM | 0.0516 mL | 0.2582 mL | 0.5164 mL | 1.2911 mL |
3CAI Related Classifications
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