AZ5104

Catalog No.S7298 Batch:S729803

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Technical Data

Formula

C27H31N7O2
Molecular Weight 485.58 CAS No. 1421373-98-9
Solubility (25°C)* In vitro DMSO 97 mg/mL (199.76 mM)
Ethanol 2 mg/mL (4.11 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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] View More
<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 Study:[1]
  • Animal Models

    Mice bearing C/L858R and C/L+T tumors

  • Dosages

    5 mg/kg/d

  • Administration

    p.o.

Selleck's AZ5104 has been cited by 4 publications

Bioanalysis of EGFRm inhibitor osimertinib, and its glutathione cycle- and desmethyl metabolites by liquid chromatography-tandem mass spectrometry. [ J Pharm Biomed Anal, 2020, 177:112871] PubMed: 31539712
YH25448, an Irreversible EGFR-TKI with Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung Cancer [ Clin Cancer Res, 2019, 25(8):2575-2587] PubMed: 30670498
Electrotaxis of Glioblastoma and Medulloblastoma Spheroidal Aggregates. [ Sci Rep, 2019, 9(1):5309] PubMed: 30926929
Activity of a novel HER2 inhibitor, poziotinib, for HER2 exon 20 mutations in lung cancer and mechanism of acquired resistance: An in vitro study. [ Lung Cancer, 2018, 126:72-79] PubMed: 30527195

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.