BI-4020 is a fourth-generation, orally active, non-covalent EGFR tyrosine kinase macrocyclic inhibitors (TKIs). It inhibits the triple mutant EGFR del19 T790M C797S mutant (IC50=0.2 nM in the BaF3 cell line), the double mutant EGFR del19 T790M, and the single mutant EGFR del19 (IC50=1 nM). and also retains activity against EGFR wt (IC50=190 nM), which can be used in studies related to non-small cell lung cancer (NSCLC).
| Molecular Weight | 542.68 |
| Formula | C30H38N8O2 |
| CAS Number | 2664214-60-0 |
| Form | Solid |
| Solubility (25°C) | DMSO > 250 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related EGFR/HER2 Products |
|---|
| Inetetamab
Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab shows antitumor activities when used alone or together with tyrosine kinase inhibitors. |
| BBT-207
BBT-207 is a reversible, mutant-specific EGFR inhibitor with antitumor activity. |
| VRN-11
VRN-11 is an EGFR C797S inhibitor. |
| TRX-221
TRX-221 is an EGFR C797S inhibitor. |
| TAS-3351
TAS-3351 is an EGFR C797S inhibitor. |
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