2. PROTAC PI3K/Akt/mTOR
  3. PROTACs Akt
  4. INY-03-041

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively.

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

INY-03-041 Chemical Structure

INY-03-041 Chemical Structure

CAS No. : 2503017-97-6

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1 mg USD 790 In-stock
5 mg USD 1750 In-stock
10 mg USD 2800 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively[1].

IC50 & Target[1]

Akt1

2.0 nM (IC50)

Akt3

3.5 nM (IC50)

Akt2

6.8 nM (IC50)

Cereblon

 

In Vitro

INY-03-041 (10-1000 nM; 0-24 hours) induces potent degradation of all three AKT isoforms in MDA-MB-468 cells[1].
INY-03-041 exhibits potent in vitro inhibition of S6K1 (IC50 =37.3 nM) and PKG1 (IC50 = 33.2 nM)[1].
INY-03-041 displays enhanced anti-proliferative effects compared with Ipatasertib (HY-15186) in MDA-MB-468 and HCC1937 cells[1].
INY-03-041 (250 nM, 12 h) promotes sustained AKT degradation and inhibition of downstream signaling effects for up to 96 h, even after compound washout[1].

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

INY-03-041 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 10 nM, 50 nM, 100 nM, 250 nM, 500 nM, 1000 nM
Incubation Time: 2 hours, 4 hours, 6 hours, 8 hours, 10 hours, 12 hours, 24 hours
Result: Induced potent degradation of all three AKT isoforms in a dose-dependent manner after a 12-h treatment, with maximal degradation observed between 100 and 250 nM. At concentrations of 500 nM and greater, AKT degradation is diminished. Treatment with 250 nM of INY-03-041 over time reveals partial degradation of all AKT isoforms within 4 h and progressive loss of AKT abundance out to 24 h.
Molecular Weight

798.41

Formula

C44H56ClN7O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N(CC1=C2C=CC=C1CCCCCCCCCCNC[C@H](C3=CC=C(Cl)C=C3)C(N4CCN(C5=C([C@H](C)C[C@H]6O)C6=NC=N5)CC4)=O)C2=O)CC7)NC7=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 115 mg/mL (144.04 mM; ultrasonic and warming and heat to 80°C; 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 1.2525 mL 6.2624 mL 12.5249 mL
5 mM 0.2505 mL 1.2525 mL 2.5050 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 5.75 mg/mL (7.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2525 mL 6.2624 mL 12.5249 mL 31.3122 mL
5 mM 0.2505 mL 1.2525 mL 2.5050 mL 6.2624 mL
10 mM 0.1252 mL 0.6262 mL 1.2525 mL 3.1312 mL
15 mM 0.0835 mL 0.4175 mL 0.8350 mL 2.0875 mL
20 mM 0.0626 mL 0.3131 mL 0.6262 mL 1.5656 mL
25 mM 0.0501 mL 0.2505 mL 0.5010 mL 1.2525 mL
30 mM 0.0417 mL 0.2087 mL 0.4175 mL 1.0437 mL
40 mM 0.0313 mL 0.1566 mL 0.3131 mL 0.7828 mL
50 mM 0.0250 mL 0.1252 mL 0.2505 mL 0.6262 mL
60 mM 0.0209 mL 0.1044 mL 0.2087 mL 0.5219 mL
80 mM 0.0157 mL 0.0783 mL 0.1566 mL 0.3914 mL
100 mM 0.0125 mL 0.0626 mL 0.1252 mL 0.3131 mL
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INY-03-041 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:

INY-03-0412503017-97-6PROTACsAktPKBProtein kinase BAKT1AKT2AKT3LenalidomideGDC-0068anti-proliferativeCRBNMDA-MB-468HCC1937 cellsZR-75-1 cellsPC3 cellsInhibitorinhibitorinhibit

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