AZ5104

Catalog No.S7298

For research use only.

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

CAS No. 1421373-98-9

Selleck's AZ5104 has been cited by 4 Publications

Purity & Quality Control

Choose Selective EGFR Inhibitors

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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

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]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.

30mg/mL

* 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
Formula

C27H31N7O2

CAS No. 1421373-98-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCN(C)C1=CC(=C(C=C1NC(=O)C=C)NC2=NC=CC(=N2)C3=CNC4=CC=CC=C43)OC

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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
NCT05120349 Not yet recruiting Drug: Osimertinib|Drug: Placebo Non-Small Cell Lung Cancer AstraZeneca January 30 2022 Phase 3
NCT04606771 Recruiting Drug: Osimertinib + Savolitinib|Drug: Savolitinib + Placebo Non-Small Cell Lung Cancer AstraZeneca September 28 2020 Phase 2
NCT02923947 Active not recruiting Drug: Osimertinib; AZD9291 Solid Tumours AstraZeneca|Quintiles Inc. May 4 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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