| Description | BAY-069 is an inhibitor. BAY-069 inhibited branched-chain amino acid transaminase 1 (BCAT1) at IC50:31 nM and branched-chain amino acid transaminase 2 (BCAT2) at IC50:153 nM. BAY-069 is a novel (trifluoromethyl) pyrimidine dione chemical probe, which can be used for anticancer research. |
| In vitro | BAY-069, inhibits the proliferation of U-87 and MDA-MB-231 cells. The compound is tested at concentrations ranging from 70 nM to 50 μM, with a duration of 72 hours. In U-87 cells, the IC50 is determined to be 358 nM, while in MDA-MB-231 cells, the IC50 is 874 nM [1]. |
| In vivo | BAY-069 demonstrates high metabolic stability when incubated with human liver microsomes, with a blood clearance of 0.11 L/h/kg. It also shows moderate metabolic stability when incubated with rat hepatocytes, with a blood clearance of 1.8 L/h/kg. BAY-069 exhibits high permeability through Caco-2 cell monolayers without any signs of efflux [1]. |
| Target activity | BCAT2:153 nM, BCAT1:31 nM |
| molecular weight | 446.81 |
| Molecular formula | C22H14ClF3N2O3 |
| CAS | 2639638-66-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 27.5 mg/mL (61.55 mM) |
| References | 1. Günther J, et al. BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe. J Med Chem. 2022;65(21):14366-14390. |