RBN012759 (500 mg/kg BID; p.o.) is well-tolerated in mice with repeat dosing[1]. RBN012759 (100 mg/kg; p.o.) exhibits moderate orally bioavailability (30%) and short plasma half-life (0.4 h) due to moderate clearance (54 mL/min/kg) and low steady-state volume of distribution (1.4 L/kg) in mice[1].
In Vitro
RBN012759 (0.01-10 μM) decreases the MAR/PAR signal corresponding to PARP14 self MARylation and stabilizes PARP14 protein in a dose-dependent manner in human primary macrophages[1]. RBN012759 (0.1-10 μM) reduces IL-4 stimulated cytokine secretion in human primary macrophages[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Schenkel L, et, al. A potent and selective PARP14 inhibitor decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants. AACR Annual Meeting 2020
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