2. PI3K/Akt/mTOR
  3. Akt
  4. 3CAI

3CAI is a potent and specific AKT1 and AKT2 inhibitor.

For research use only. We do not sell to patients.

3CAI Chemical Structure

3CAI Chemical Structure

CAS No. : 28755-03-5

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 73 In-stock
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10 mM * 1 mL in DMSO USD 73 In-stock
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10 mg USD 106 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

3CAI Related Antibodies

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Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

3CAI is a potent and specific AKT1 and AKT2 inhibitor.

IC50 & Target[1]

Akt1

 

Akt2

 

In Vitro

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.

3CAI Related Antibodies
In Vivo

To examine the antitumor activity of 3CAI in vivo, HCT116 cancer cells are injected into the right flank of individual athymic nude mice. Mice are orally administered 3CAI at 20 or 30 mg/kg, I3C at 100 mg/kg, or vehicle 5 times a week for 21 days. Treatment of mice with 30 mg/kg of 3CAI significantly suppresses HCT116 tumor growth by 50% relative to the vehicle-treated group (p<0.05). Remarkably, mice seem to tolerate treatment with these doses of 3CAI without overt signs of toxicity or significant loss of body weight compared with vehicle-treated group. Expression of these AKT-target proteins is strongly suppressed by 30 mg/kg of 3CAI in tumor tissues[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

193.63

Formula

C10H8ClNO
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(CCl)C1=CNC2=CC=CC=C12
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.1645 mL 25.8224 mL 51.6449 mL
5 mM 1.0329 mL 5.1645 mL 10.3290 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (10.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
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3CAI Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

3CAI28755-03-5AktPKBProtein kinase BInhibitorinhibitorinhibit

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