AZD8835 - 98%, high purity , CAS No.1620576-64-8, Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta;Inhi

Item Number

A413893

• Synonyms: BDBM185362 | UNII-8B97A88D35 | CCG-269444 | compound 25 [PMID: 26475521] | NCGC00484075-01 | 1-(4-{5-[5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl]-1-ethyl-1H-1,2,4-triazol-3-yl}piperidin-1-yl)-3-hydroxypropan-1-one | CS-4984 | Z2327409009 |
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
• Storage Temp: Store at -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta;Inhi

Product Description

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