BI-4020 is a highly active, non-covalent EGFR inhibitor (IC50 = 0.6 nM). BI-4020 displays a single digit-nanomolar antiproliferative activity against EGFR mutant dependent cells, including cells which are dependent on EGFR bearing the two most clinically prevalent resistance mutations T790M and C797S. At the same time BI-4020 shows a sufficient EGFRwt sparing window and high kinome selectivity that is comparable to the one observed with osimertinib. Furthermore BI-4020 induces tumor regressions in the osimertinib resistant PC-9 (EGFRdel19 T790M C797S) triple mutant mouse xenograft model.
MedKoo Cat#: 407046
Name: BI-4020
CAS#: Unknown
Chemical Formula: C30H38N8O2
Exact Mass: 542.3118
Molecular Weight: 542.69
Elemental Analysis: C, 66.40; H, 7.06; N, 20.65; O, 5.90
The following data is based on the product molecular weight 542.69 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
