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UNC2881

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Chemical Structure| 1493764-08-1 同义名 : -
CAS号 : 1493764-08-1
货号 : A214490
分子式 : C25H33N7O2
纯度 : 99%+
分子量 : 463.575
MDL号 : MFCD28142814
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(97.07 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Mer is a member of the TAM (Tyro3, Axl and Mer) receptor tyrosine kinase (RTK) subfamily with growth-arrest-specific-6 (Gas6) as one of the endogenous ligands. Elevated Mer activation has been strongly associated with the oncogenesis of a number of human cancers. Recently, Mer has also been shown to play important roles in regulating macrophage activity and platelet aggregation[2]. UNC2881 is a specific Mer tyrosine kinase inhibitor with an IC50 of 4.3 nM, and its selectivity is 83-fold and 58-fold higher than that of Axl and Tyro3, respectively[2]. When applied to live cells, UNC2881 inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. Treatment with UNC2881 is also sufficient to block EGF (epidermal growth factor)-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[2]. In mice, UNC2881 had high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability. The terminal half-life was 0.80 h. The volume of distribution was 2-fold greater than the normal volume of total body water (0.70 L/kg)[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
697 B-ALL cells Function assay 1 h Inhibition of Mer kinase phosphorylation in human 697 B-ALL cells after 1 hr by Western blot analysis, IC50=0.022 μM 24219778
mouse 32D-EMC cells Function assay Inhibition of EGF-induced human intracellular domain of Mer/extracellular domain of EGFR phosphorylation expressed in mouse 32D-EMC cells after 1 hr by Western blot analysis 24219778
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.57mL

4.31mL

2.16mL
参考文献

[1]Zhang W, McIver AL, et al. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem. 2013 Dec 12;56(23):9693-700.

[2]Zhang W, McIver AL, Stashko MA, DeRyckere D, Branchford BR, Hunter D, Kireev D, Miley MJ, Norris-Drouin J, Stewart WM, Lee M, Sather S, Zhou Y, Di Paola JA, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem. 2013 Dec 12;56(23):9693-700. doi: 10.1021/jm4013888. Epub 2013 Nov 20. PMID: 24219778; PMCID: PMC3962266.