AZ5104

Catalog No.S7298

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.
Targets
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]

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • Animal Models: Mice bearing C/L858R and C/L+T tumors
  • Formulation: 1% Polysorbate 80
  • 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 individually and in order:
1% Tween 80
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 powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID