2. PI3K/Akt/mTOR
  3. Akt
  4. Akt3 degrader 1

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。

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Akt3 degrader 1 Chemical Structure

Akt3 degrader 1 Chemical Structure

CAS No. : 2836342-69-7

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Akt3 degrader 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target

Akt3[1].
体外研究
(In Vitro)

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].

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

Akt3 degrader 1 相关抗体:

Cell Proliferation Assay[1]

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[1]

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.
体内研究
(In Vivo)

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].

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

Animal Model: NOD-SCID-IL2Rg-/-(NSI) mice (H1975OR xenograft model)[1].
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.
分子量

885.19

Formula

C53H72N8O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Akt3 degrader 1 相关分类

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Keywords:

Akt3 degrader 12836342-69-7AktPKBProtein kinase BNSCLCosimertinib resistanceA549HCC827H1975H1975ORPC9H1299H460Inhibitorinhibitorinhibit

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目录号：
HY-151606
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