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CAS No.: 1493764-08-1

UNC2881 Catalog No. CSN16090

Synonyms: UNC2881

UNC2881 is a Mer kinase inhibitor and can inhibit the phosphorylation of Mer with IC50 of 4.3 nM.

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生物活性

实验方案

技术信息

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1571 mL
- 10.7857 mL
- 21.5715 mL
- 5 mM
- 0.4314 mL
- 2.1571 mL
- 4.3143 mL
- 10 mM
- 0.2157 mL
- 1.0786 mL
- 2.1571 mL

技术信息

CAS号

1493764-08-1

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H33N7O2

运输

蓝冰

分子量

463.58

别名

UNC2881

溶解度

DMSO	155.0 mg/mL (334.4 mM) warming
Water	insoluble

动物实验配方

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