| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (6.8 mM), Sonication is recommended.
Ethanol : 16 mg/mL (32.95 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 250 mg/mL (514.85 mM), Sonication is recommended.
|
| Keywords | Inhibitor | inhibit | HER2/ErbB2 | HER1 | ErbB-1 | Epidermal growth factor receptor | EGFR (wildtype) | EGFR (L861Q) | EGFR (L858R/T790M) | EGFR (L858R) | EGFR | AZ-5104 | AZ5104 | AZ 5104 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | JAK-STAT Compound Library | Inhibitor Library | NO PAINS Compound Library | Immuno-Oncology Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max |
United States
