CAS NO: | 1493764-08-1 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
10mg | 电议 |
50mg | 电议 |
Cas No. | 1493764-08-1 |
Canonical SMILES | O[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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |