Name | AZ-5104 |
Description | AZ5104 is a potent EGFR inhibitor. |
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 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] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : 16 mg/mL (33 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 90 mg/mL (185.3 mM)
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Keywords | AZ 5104 | Epidermal growth factor receptor | HER1 | AZ-5104 | EGFR | ErbB-1 | inhibit | AZ5104 | Inhibitor |
Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
Related Compound Libraries | Reprogramming Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Anti-Prostate Cancer Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library |