product name UNC2881
Description: UNC2881 is a potent and specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively. UNC2281 inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. Treatment with UNC2281 is also sufficient to block EGF-mediated stimulation of a chimeric receptor containing the intracellular domain of Mer fused to the extracellular domain of EGFR. In addition, UNC2881 potently inhibits collagen-induced platelet aggregation, suggesting that this class of inhibitors may have utility for prevention and/or treatment of pathologic thrombosis.
References: J Med Chem. 2013 Dec 12;56(23):9693-700.
463.58
Formula
C25H33N7O2
CAS No.
1493764-08-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 292 mg/mL (198.5 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL (10.8 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: UNC2881 inhibits Mer kinase activity in 697 B-ALL cells with IC50 of 22 nM, and inhibits collagen-stimulated platelet aggregation. Kinase Assay: Cell Assay: 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. |
|---|---|
| In Vivo | UNC2881 have high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability in mice. |
| Animal model | Mouse model |
| Formulation & Dosage | |
| References | J Med Chem. 2013 Dec 12;56(23):9693-700. |
