| Description | BI-0474 is a potent KRASG12C inhibitor that inhibits GDP-KRAS::SOS1 protein-protein interactions with an IC50 value of 7.0 nM.BI-0474 exhibits significant antiproliferative activity against NCI-H358 cells harboring the G12C mutation, and shows significant anti-tumor activity in a non-small cell lung cancer xenograft model. activity.BI-0474 can be used for cancer research. |
| In vitro | BI-0474 (1-10,000 nM; 3 days; NCI-H358 cells carrying a G12C mutation) inhibited proliferation of NCI-H358 cells with an EC50 of 26 nM.[1] |
| In vivo | BI-0474 (40 mg/kg; i.p.; single daily for 3 days; NMRI nude mice) shows anti-tumor efficacy and pharmacodynamic biomarker modulation. This led to the induction of programmed cell death in this xenograft model.[1] |
| Target activity | KRAS-SOS1:7 nM |
| molecular weight | 587.74 |
| Molecular formula | C30H37N9O2S |
| CAS | 2750570-55-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Bröker J, et al. Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor. J Med Chem. 2022 Oct 27. |