规格: | 98% |
分子量: | 378.46 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Background:
RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of<3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants[1].
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].
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].
[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.