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UNC2881
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。
UNC2881图片
CAS NO:1493764-08-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
UNC2881 是一种具有口服活性的特异性 Mer 激酶抑制剂,抑制稳态 Mer 激酶磷酸化,IC50 值为 22 nM。
Cas No.1493764-08-1
Canonical SMILESO[C@H]1CC[C@H](CC1)NC2=NC(NCCCC)=NC=C2C(NCC(C=C3)=CC=C3N4C=CN=C4)=O
分子式C25H33N7O2
分子量463.58
溶解度≥ 13.55mg/mL in DMSO
储存条件Store at -20℃
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

UNC2881 is a selective inhibitor of Mer tyrosine kinase [1].

Mer is a member of the TAM (Tyro3, Axl and Mer) receptor tyrosine kinase (RTK) subfamily with growth-arrest-specific-6 (Gas6) as an endogenous ligand. Mer plays an important role in platelet aggregation and macrophage activity.

UNC2881 is a novel and specific Mer tyrosine kinase inhibitor. In kinase inhibition assays, UNC2881 (430 nM) inhibited MER, FGFR1, KDR, EGFR, ITK and TRKA by greater than 50%. In 697 B-ALL cells, UNC2881 inhibited Mer phosphorylation with IC50 value of 22 nM. Also, UNC2881 inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the intracellular domain of Mer and the extracellular domain of the epidermal growth factor receptor (EGFR). In human platelet-rich plasma, UNC2881 inhibited platelet aggregation induced by fibrillar Type I equine collagen by greater than 25%. UNC2881 also inhibited ATP release, a marker of platelet activation [1].

In mice, UNC2881 exhibited 14% oral bioavailability and high systemic clearance. UNC2881 was sufficient for in vitro or short-term in vivo studies [1].

Reference:
[1].  Zhang W, McIver AL, Stashko MA, et al. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem, 2013, 56(23): 9693-9700.