Home PI3K/Akt/mTOR PI3K inhibitor AZD8835 For research use only.

AZD8835

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

AZD8835 Chemical Structure

CAS No. 1620576-64-8

Purity & Quality Control

Batch: S796601 DMSO]93 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.01%
99.01

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Signaling Pathway

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PI3K Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models CD1 mice
Dosages 0.1 mL/10 g mouse
Administration oral administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02260661 Completed
Advanced Solid Malignancies|Breast Cancer - ER+ HER2 -|Breast Cancer - ER+ HER2- PIK3CA Gene Mutation
AstraZeneca
 November 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 469.54 Formula

C22H31N9O3
CAS No. 1620576-64-8 SDF Download AZD8835 SDF
Smiles CCN1C(=NC(=N1)C2CCN(CC2)C(=O)CCO)C3=CN=C(C(=N3)C4=NN=C(O4)C(C)(C)C)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (198.06 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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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