UNC2881 |
Catalog No.GC13500 |
UNC2881 es un inhibidor de la quinasa Mer especÍfico activo por vÍa oral que inhibe la fosforilaciÓn de la quinasa Mer en estado estacionario con un valor IC50 de 22 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1493764-08-1
Sample solution is provided at 25 µL, 10mM.
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.
Average Rating: 5
(Based on Reviews and 33 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *