中文名：AZD8835
英文名：AZD8835
纯度：Moligand™，≥98%
货号：A413893
Cas号：1620576-64-8
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
AZD8835 ia a novel mixed inhibitor ofPI3KαandPI3Kδwith IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity againstPI3Kβ(IC50=431 nM) andPI3Kγ(IC50=90 nM).
Targets
PI3Kδ (Cell-based assay); PI3Kα (Cell-free assay); PI3Kγ (Cell-based assay); PI3Kβ (Cell-based assay) 5.7 nM; 6.2 nM; 90 nM; 431 nM
In vitro
AZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H1047R mutations) and PI3Kδ with excellent selectivity vs. PI3Kβ, PI3Kγ and an excellent general kinase selectivity. AZD8835 is a potent inhibitor of p-Akt in cells sensitive to PI3Kα inhibition (IC50=0.057 μM in PIK3CA mutant human breast ductal carcinoma BT474 cell line) and in cells sensitive to PI3Kδ inhibition (IC50=0.049 μM in JeKo-1 B cell line), but not to cells sensitive to PI3Kβ inhibition (IC50=3.5 μM in PTEN breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line).
In vivo
AZD8835 has antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously and displays high metabolic stability and suitable physical properties for oral administration.
Cell Research(from reference)
Cell lines：BT474, MCF7, or T47D cells
Concentrations：250 nmol/L
Incubation Time：24 h
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关键字： BDBM185362 ; UNII-8B97A88D35 ; CCG-269444 ; compound 25 [PMID: 26475521]
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