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CAS No.: 1493694-70-4

UNC2250 Catalog No. CSN16916

Synonyms: UNC2250

UNC2250 is an inhibitor of Mer with IC50 of 1.7 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Mer

IC50:1.7nM
描述Mer belongs to the TAM (Tyro3, Axl, Mer) family of receptor tyrosine kinases (RTK). This subfamily of RTKs transduce signals from the extracellular matrix into the cytoplasm by binding to several ligands including LGALS3, TUB, TULP1 or GAS6. Abnormal activation or overexpression of Mer RTK has been implicated in neoplastic progression of many human cancers and has been correlated with poorer prognosis. UNC2250 is a Mer kinase inhibitor which achieved selectivity against the other two members of Tyro3 and Axl. Based on a microfluidic capillary electrophoresis assay, the IC50 of UNC2250 against Mer was 1.7 nM, while the IC50s against Axl and Tyro3 were 270 nM and 100 nM, respectively ^[2]. UNC2250 inhibited Mer phosphorylation with the IC50 value of 9.8 nM as detected by western blotting^[2]. In soft agar colony formation assays, UNC2250 inhibited colony formation of the BT-12 rhabdoid tumor and the NSCLC Colo699 cells^[2]. According to another report, UNC2250 inhibited proliferation of the mantle cell lymphoma cell lines Z-138, Mino, and JVM-13 with IC50 values of 3.0 μM, 3.1 μM and 7.7 μM, respectively^[3]. In an apoptosis assay, flow cytometry analysis revealed that 4 μM UNC2250 induced apoptosis in Z-138 cells by 45.2% and Mino cells by 44.4% post 12h treatment, and when the time was extended to 24 or 48h, the apoptosis rates induced by 4 μM UNC2250 increased to 76.9 or 98.0% in Z-138 cells and to 81.5 or 98.1% in Mino cells^[3]. In an mantle cell lymphoma Z-138 xenograft model established on NOD/SCID mice, UNC2250 was administrated once daily by oral gavage for 10 days. UNC2250 produced significant anti-tumor effects on tumor volume at the doses of 50 and 75 mg/kg. The tumor inhibition rates were 35 and 48%, respectively^[3].
动物研究
剂量
Mouse: 3 mg/kg^[2] (i.v.); 25 mg/kg - 75 mg/kg^[3] (p.o., qd)

给药途径
i.v., p.o.
参考文献

动物研究
剂量	Mouse: 3 mg/kg^[2] (i.v.); 25 mg/kg - 75 mg/kg^[3] (p.o., qd)
给药途径	i.v., p.o.

[1] Zhang W, Zhang D, et al. Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem. 2013 Dec 12;56(23):9683-92.
[2] Zhang W, Zhang D, Stashko MA, DeRyckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem. 2013 Dec 12;56(23):9683-92. doi: 10.1021/jm401387j. Epub 2013 Nov 20. Erratum in: J Med Chem. 2014 Aug 28;57(16):7141. PMID: 24195762; PMCID: PMC3980660.
[3] Shi C, Li X, Wang X, Ding N, Ping L, Shi Y, Mi L, Lai Y, Song Y, Zhu J. The proto-oncogene Mer tyrosine kinase is a novel therapeutic target in mantle cell lymphoma. J Hematol Oncol. 2018 Mar 20;11(1):43. doi: 10.1186/s13045-018-0584-6. PMID: 29554921; PMCID: PMC5859520.

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
- 2.2697 mL
- 11.3486 mL
- 22.6973 mL
- 5 mM
- 0.4539 mL
- 2.2697 mL
- 4.5395 mL
- 10 mM
- 0.2270 mL
- 1.1349 mL
- 2.2697 mL

技术信息

CAS号

1493694-70-4

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H36N6O2

运输

蓝冰

分子量

440.58

别名

UNC2250

溶解度

DMSO	2.0 mg/mL (4.5 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+30% PEG 300+water

0.5 mg/mL

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UNC2250 Catalog No. CSN16916

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