| Name | BI-4020 |
| Description | BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties. |
| In vitro | BI-4020 inhibits p-EGFR del19 T790M C797S (IC50: 0.6 nM) and the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines), as well as the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM), with activity against EGFR wt (IC50: 190 nM), and exhibits high kinome selectivity and good DMPK properties. |
| In vivo | In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 240 mg/mL (442.25 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.21 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | HER1 | ErbB-1 | Epidermal growth factor receptor | EGFRWT | EGFRdel19 T790M C797S | EGFRdel19 T790M | EGFRdel19 | EGFR (wt) | EGFR (del19/T790M/C797S) | EGFR (del19/T790M) | EGFR (del19) | EGFR | BI-4020 | BI4020 | BI 4020 |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Cytokine Inhibitor Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Hematonosis Compound Library | Angiogenesis related Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
