Akt3 degrader 1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Akt3 degrader 1 (化合物 12l) 是一种选择性的 Akt3 降解剂，能克服 Osimertinib (HY-15772) 诱导的 H1975OR NSCLC 细胞的抗性。Akt3 degrader 1 还具有抗增殖活性，能显著抑制小鼠体内肿瘤的生长。Akt3 degrader 1 可用于耐药性非小细胞肺癌的研究。

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.

Akt3 degrader 1 (0.001-100 μM; 24 h) shows antiproliferative effects on H1975OR cells with an IC50 of 0.972 μM.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.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.Akt3 degrader 1 overcomes osimertinib-induced resistance in H1975OR NSCLC cells via disrupting the noncatalytic functions of Akt3.Cell Proliferation Assay Cell Line:H1975OR cells Concentration:0.001-100 μM Incubation Time:24 h Result:Inhibited growth of H1975OR cells with an IC50 of 0.972 μM.Western Blot Analysis Cell Line:A549, HCC827, H1975, H1975OR, PC9, H1299, and H460 cells Concentration:1.6, 8, 40, 200, 1000 nM Incubation Time:24 h Result:Selectively induced Akt3 degradation in all of these cell lines in a dose-dependent manner, whereas had minimal influence on Akt1 and Akt2 protein levels.

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.Animal Model:NOD-SCID-IL2Rg-/-(NSI) mice (H1975OR xenograft model).Dosage:10, 20 mg/kg Administration:Intraperitoneal administration; every 3 days for 5 weeks Result:Inhibited tumor growth without causing obvious body weight loss or other signs of toxicity.

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Cytoskeleton/Cell Adhesion Molecules

Akt

Akt

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2836342-69-7

885.19

C53H72N8O4

>98% (HPLC)

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O=C1C=C(C=2C=NC(=NC2N1C=3C=CC=C(C3)NC(=O)C4CC4)NC5=CC=C(C=C5OC)N6CCN(CC6)CCCCCCCCCCCCNC(=O)CC78CC9CC(CC(C9)C7)C8)C

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(-20℃)

With Ice Pack

≥ 2 years