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RBN012759
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RBN012759图片
规格:98%
分子量:378.46
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
RBN012759 是一种有效的,选择性和具有口服活性的 PARP14 抑制剂,IC50 值<3 nm,比对 monoparps 的选择性高 300 倍,比对 polyparps 1000 倍。rbn012759 可以降低肿瘤前巨噬细胞的功能并引起肿瘤外植体的炎症反应。
货号:ajcx33790
CAS:2360851-29-0
分子式:C19H23FN2O3S
分子量:378.46
溶解度:DMSO : 250 mg/mL (660.57 mM; Need ultrasonic)
纯度:98%
存储:Store at -20°C
库存:现货

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.