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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
CAS NO:2360851-29-0
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
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 的选择性高 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。
Cas No.2360851-29-0
分子式C19H23FN2O3S
分子量378.46
溶解度DMSO : 250 mg/mL (660.57 mM; Need ultrasonic)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.