AZD8835

Catalog No.S7966

AZD8835 Chemical Structure

Molecular Weight(MW): 469.54

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).

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Biological Activity

Description 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).
Targets
PI3Kδ [2]
(Cell-based assay)
PI3Kα [2]
(Cell-free assay)
PI3Kγ [2]
(Cell-based assay)
PI3Kβ [2]
(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 null breast adenocarcinoma MDA-MB-468 cell line) or PI3Kγ inhibition (IC50=0.53 μM in monocytic RAW264 cell line)[2].

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[1][2].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: BT474, MCF7, or T47D cells
  • Concentrations: 250 nmol/L
  • Incubation Time: 24 h
  • Method: BT474, MCF7, or T47D cells are seeded in 384-well plates at a density of 500 to 2,000 cells per well and incubated overnight. Cells are dosed with compound(s) and cell confluency is measured at 4-hour intervals over several days.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: CD1 mice
  • Formulation: a suspension in HPMC/Tween [0.5% hydroxypropyl methocellulose (Methocel (Colocorn))/0.1% Polysorbate 80]
  • Dosages: 0.1 mL/10 g mouse
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 93 mg/mL (198.06 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 469.54
Formula

C22H31N9O3

CAS No. 1620576-64-8
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID