UNC2881

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

UNC2881 是一种特异性 Mer 酪氨酸激酶抑制剂 (IC50: 4.3 nM)。其选择性分别比 Axl 和 Tyro3 高约 83 倍和 58 倍。

UNC2881 is a potent Mer kinase inhibitor. 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.

UNC2881 (compound 23) (0-1000 nM; 1 h) block ligand-stimulated activation of a chimeric EGFR-MerTK. UNC2881 also inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells. UNC2881 (3 μM; 1 h) suppresses platelet aggregation by greater than 25% in human platelet-rich plasma in response to stimulation with fibrillar type I equine collagen. Western Blot Analysis Cell Line:32D cells Concentration:0, 10, 30, 100, 300, 1000 nM Incubation Time:1 hour; prior to stimulation with 100 ng/mL EGF ligand for 15 min Result:Reduced the phospho-tyrosine level in a dose-dependent manner.

UNC2881 (3 mg/kg; p.o.; single dose) has high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability, displays terminal half-life of 0.80 h.UNC2881 (3 mg/kg; i.v.; injected with VSV on days -3, -2, -1, and 0) limits Mertk signaling, and promotes the antiviral immune response, reducing the viral replication of vesicular stomatitis virus (VSV) in infected mice.Pharmacokinetics of UNC2881 in mice Animal Model:C57BL/6 mice (7-10 weeks old)Dosage:3 mg/kg Administration:Intravenous injection; infected with 2×108 PFU vesicular stomatitis virus (VSV) (i.v.) on days -3, -2, -1, and 0Result:Reduced VSV replication in spleen, liver, kidney, lung.

UNC2881, UNC-2881, UNC 2881

Endocrinology/Hormones

AChR

AXL| Mer| Tyro3

Cardiovascular Disease

——

1493764-08-1

463.58

C25H33N7O2

>98% (HPLC)

DMSO : ≥ 44 mg/mL; 94.91 mM

CCCCNc1ncc(c(N[C@@H]2CC[C@H](CC2)O)n1)C(=O)NCc1ccc(n2ccnc2)cc1

N-(4-(1H-imidazol-1-yl)benzyl)-2-(butylamino)-4-(((1r,4r)-4-hydroxycyclohexyl)amino)pyrimidine-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years