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