AZD8835

Catalog No.S7966

For research use only.

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).

AZD8835 Chemical Structure

CAS No. 1620576-64-8

Selleck's AZD8835 has been cited by 2 Publications

Purity & Quality Control

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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 (from reference)

Cell Research:[1]
  • 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.
Animal Research:[1]
  • Animal Models: CD1 mice
  • Dosages: 0.1 mL/10 g mouse
  • Administration: oral administration

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 469.54
Formula

C22H31N9O3

CAS No. 1620576-64-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C(=NC(=N1)C2CCN(CC2)C(=O)CCO)C3=CN=C(C(=N3)C4=NN=C(O4)C(C)(C)C)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02260661 Completed Drug: AZD8835|Drug: AZD8835 in combination with fulvestrant Advanced Solid Malignancies|Breast Cancer - ER+ HER2 -|Breast Cancer - ER+ HER2- PIK3CA Gene Mutation AstraZeneca November 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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

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