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AZD8835 PI3K inhibitor

Cat.No.S7966

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 PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 469.54

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (198.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Chemical Information, Storage & Stability

Molecular Weight 469.54 Formula

C22H31N9O3

 Storage (From the date of receipt)
CAS No. 1620576-64-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCN1C(=NC(=N1)C2CCN(CC2)C(=O)CCO)C3=CN=C(C(=N3)C4=NN=C(O4)C(C)(C)C)N

Mechanism of Action

Targets/IC50/Ki
PI3Kδ
(Cell-based assay)
5.7 nM
PI3Kα
(Cell-free assay)
6.2 nM
PI3Kγ
(Cell-based assay)
90 nM
PI3Kβ
(Cell-based assay)
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. This compound 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).
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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