2. PI3K/Akt/mTOR
  3. Akt
  4. AKT-IN-1

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.

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

AKT-IN-1 Chemical Structure

AKT-IN-1 Chemical Structure

CAS No. : 1357158-81-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
1 mg USD 142 In-stock
5 mg USD 300 In-stock
10 mg USD 510 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

AKT-IN-1 Related Antibodies

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Description

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.

IC50 & Target

IC50: 1.042 μM (AKT)[1]
In Vitro

AKT-IN-1 is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40[1].

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

AKT-IN-1 Related Antibodies
In Vivo

The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition[1].

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

343.42

Formula

C22H21N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(C1=CN=C(C2=CC=C(C3(N)CCC3)C=C2)C(C4=CC=CC=C4)=C1)=O
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 : 75 mg/mL (218.39 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 2.9119 mL 14.5594 mL 29.1189 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 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
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 2.5 mg/mL (7.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

Purity: 98.41%

COA (251 KB) LCMS (267 KB)

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 2.9119 mL 14.5594 mL 29.1189 mL 72.7972 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL 14.5594 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 mL 7.2797 mL
15 mM 0.1941 mL 0.9706 mL 1.9413 mL 4.8531 mL
20 mM 0.1456 mL 0.7280 mL 1.4559 mL 3.6399 mL
25 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9119 mL
30 mM 0.0971 mL 0.4853 mL 0.9706 mL 2.4266 mL
40 mM 0.0728 mL 0.3640 mL 0.7280 mL 1.8199 mL
50 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4559 mL
60 mM 0.0485 mL 0.2427 mL 0.4853 mL 1.2133 mL
80 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9100 mL
100 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7280 mL
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AKT-IN-1 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:

AKT-IN-11357158-81-6AktPKBProtein kinase BInhibitorinhibitorinhibit

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