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UNC2881

In stock
Catalog No.
B4357
Mer tyrosine kinase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$150.00
In stock
10mg
$155.00
In stock
50mg
$635.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt463.58
Cas No.1493764-08-1
FormulaC25H33N7O2
Solubility≥13.55mg/mL in DMSO
SDFDownload SDF
Canonical SMILESO[[email protected]]1CC[[email protected]](CC1)NC2=NC(NCCCC)=NC=C2C(NCC(C=C3)=CC=C3N4C=CN=C4)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description UNC2881 is a specific inhibitor of Mer tyrosine kinase with IC50 value of 4.3 nM.
Targets Mer tyrosine kinase          
IC50 4.3 nM          

Quality Control

Chemical structure

UNC2881