Akt3 degrader 1 

Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer^[1].

Akt3^[1].

Akt3 degrader 1 (0.001-100 µM; 24 h) shows antiproliferative effects on H1975OR cells with an IC₅₀ of 0.972 µM^[1].
Akt3 degrader 1 (1.6, 8, 40, 200, 1000 nM; 24 h) induces degradation of Akt3 through the ubiquitin proteasome-mediated proteolysis process in NSCLC cell lines^[1].
Akt3 degrader 1 (10, 100 nM) selectively and dose-dependently degrades exogenous PH domain-only Akt3 protein but not the Akt3 del PH mutant in H1975OR cells^[1].
Akt3 degrader 1 overcomes osimertinib-induced resistance in H1975OR NSCLC cells via disrupting the noncatalytic functions of Akt3^[1].

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

Akt3 degrader 1 (10, 20 mg/kg; i.p.; every 3 days for 5 weeks) induces significant tumor growth inhibition (TGI) with an approximately TGI value of 75% in mice^[1].

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

885.19

C₅₃H₇₂N₈O₄

2836342-69-7

COC1=C(C=CC(N2CCN(CC2)CCCCCCCCCCCCNC(CC34CC5CC(C4)CC(C3)C5)=O)=C1)NC6=NC=C7C(C)=CC(N(C7=N6)C8=CC=CC(NC(C9CC9)=O)=C8)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Xu F, et al. Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells. J Med Chem. 2022 Oct 27;65(20):14032-14048.  [Content Brief]