BAY-069

BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer[1].

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

IC50: 31 nM (BCAT1), 153 nM (BCAT2)[1]

BAY-069 (compound 36a) (70 nM-50 μM; 72 h) inhibits cell proliferation of U-87 and MDA-MB-231[1]. Cell Proliferation Assay[1] Cell Line: U-87 and MDA-MB-231 Concentration: 70 nM-50 μM Incubation Time: 72 h Result: Inhibited cell proliferation of U-87 and MDA-MB-231 with IC50s of 358 nM and 874 nM, respectively.

BAY-069 exhibits high metabolic stability after incubation with human liver microsomes (CLblood = 0.11 L/h/kg) and moderate metabolic stability after incubation with rat hepatocytes (CLblood = 1.8 L/h/kg); shows high permeability through Caco-2 cell monolayers with no hint of efflux[1]. BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2). Animal Model: Male Wistar rats[1] Dosage: 0.3 mg/kg for i.v.; 0.6 mg/kg for p.o. Administration: i.v. or p.o.; single dosage Result: Pharmacokinetic Parameters of BAY-069 in male Wistar rats[1]. CLblood (L/h/kg) Vss (L/kg) t1/2 (h), i.v. AUCnorm (kg·h/L), i.v. AUCnorm (kg·h/L), p.o. F (%), p.o. 0.64 0.25 1.6 2.9 2.5 89

[1]. Günther J, et al. BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe. J Med Chem. 2022 Oct 19.