Description | BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants. BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants with an average IC50 value of approximately 140 nM. |
In vitro | BI-2865 inhibits the proliferation of BaF3 cells expressing G12C, G12D or G12V mutant KRAS in the presence of IL-13 with a mean IC50 of approximately 140 nM.[1] |
molecular weight | 465.57 |
Molecular formula | C23H27N7O2S |
CAS | 2937327-93-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 225.0 mg/mL (483.3 mM), Sonication is recommended. |
References | 1. Kim D, et al. Pan-KRAS inhibitor disables oncogenic signalling and tumour growth. Nature. 2023;619(7968):160-166. |
Citations | 1. Guo Y, Tian J, Guo Y, et al.Oncogenic KRAS effector USP13 promotes metastasis in non-small cell lung cancer through deubiquitinating β-catenin.Cell Reports.2023, 42(12). |