For research use only.

Catalog No.S7298

4 publications

AZ5104 Chemical Structure

Molecular Weight(MW): 485.58

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.

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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.
EGFR (L858R/T790M) [1] EGFR (L861Q) [1] EGFR (L858R) [1] ErbB4 [1] EGFR (wildtype) [1]
<1 nM 1 nM 6 nM 7 nM 25 nM
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]

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]


Kinase Assay:[1]
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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.
Animal Research:[1]
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  • Animal Models: Mice bearing C/L858R and C/L+T tumors
  • Dosages: 5 mg/kg/d
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (199.76 mM)
Ethanol 23 mg/mL warmed (47.36 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% Tween 80
For best results, use promptly after mixing.

* 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 485.58


CAS No. 1421373-98-9
Storage powder
in solvent
Synonyms N/A
Smiles COC1=C(NC2=NC=CC(=N2)C3=C[NH]C4=C3C=CC=C4)C=C(NC(=O)C=C)C(=C1)N(C)CCN(C)C

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02923947 Active not recruiting Drug: Osimertinib; AZD9291 Solid Tumours AstraZeneca|Quintiles Inc. May 4 2017 Phase 1
NCT02511106 Active not recruiting Drug: AZD9291 80 mg/40 mg|Drug: Placebo AZD9291 80 mg/40 mg Stage IB-IIIA Non-small Cell Lung Carcinoma AstraZeneca October 21 2015 Phase 3
NCT02529995 Completed Drug: AZD9291 40 mg|Drug: AZD9291 80 mg Carcinoma Non-Small-Cell Lung With EGFR Mutation Positive AstraZeneca August 24 2015 Phase 1

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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.

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EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID