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INY-03-041

Catalog No.GC65559

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide (Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively.

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INY-03-041 Chemical Structure

Cas No.: 2503017-97-6

Size Price Stock Qty
1mg
$711.00
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5mg
$1,575.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Akt1

2.0nM(IC50)

Akt2

6.8nM(IC50)

Akt3

3.5nM(IC50)

Cereblon

 

Background

INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor GDC-0068 conjugated to Lenalidomide (Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0 nM, 6.8 nM and 3.5 nM, respectively[1].

INY-03-041 (10-1000 nM; 2-24 hours; MDA-MB-468 cells) treatment induces 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[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 GDC-0068 in MDA-MB-468 and HCC1937 cells[1].

[1]. You I, et al. Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling. Cell Chem Biol. 2020 Jan 16;27(1):66-73.e7.

Chemical Properties

Cas No. 2503017-97-6 SDF Download SDF
Formula C44H56ClN7O5 M.Wt 798.41
Solubility DMSO : 115 mg/mL (144.04 mM; ultrasonic and warming and heat to 80°C) Storage -20°C, away from moisture
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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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 2.505 mL
10 mM 0.1252 mL 0.6262 mL 1.2525 mL
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