Home Protein Tyrosine Kinase EGFR inhibitor AZ5104 For research use only.

AZ5104

AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.

AZ5104 Chemical Structure

AZ5104 Chemical Structure

CAS: 1421373-98-9

Selleck's AZ5104 has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.77%
99.77

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Biological Activity

Description AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
Targets
EGFR (L858R/T790M) [1] EGFR (L861Q) [1] EGFR (L858R) [1] ErbB4 [1] EGFR (wildtype) [1] Click to View More Targets
<1 nM 1 nM 6 nM 7 nM 25 nM
In vitro
In vitro AZ5104 shows great potency against ex19del (2 nM in PC-9), T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 causes inhibition of cell viability with IC50 of 3.3 nM, 2.6 nM, 80 nM, and 53 nM for H1975 (T790M/L858R), PC-9 (ex19del), Calu 3 (WT), and NCI-H2073 (WT), respectively. [1]
Kinase Assay Recombinant Kinase assays
Kinase assays are performed using peptide or protein substrates in a filter-binding radioactive ATP transferase assay for protein kinases, or lipid substrates and HTRF assay for lipid kinase.
In Vivo
In vivo In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression. [1]
Animal Research Animal Models Mice bearing C/L858R and C/L+T tumors
Dosages 5 mg/kg/d
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05748093 Not yet recruiting Non-small Cell Lung Cancer Maastricht University Medical Center June 1 2023 Phase 4
NCT05120349 Recruiting Non-Small Cell Lung Cancer AstraZeneca February 21 2022 Phase 3
NCT04606771 Active not recruiting Non-Small Cell Lung Cancer AstraZeneca September 28 2020 Phase 2

Chemical lnformation & Solubility

Molecular Weight 485.58 Formula

C27H31N7O2
CAS No. 1421373-98-9 SDF Download AZ5104 SDF
Smiles CN(C)CCN(C)C1=CC(=C(C=C1NC(=O)C=C)NC2=NC=CC(=N2)C3=CNC4=CC=CC=C43)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (199.76 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : 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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