|1-(6-(3,5-二氯-4-羟基苯基)-4-((反式-4-((二甲基氨基)甲基)环己基)氨基)-1,5-萘啶-3-基)乙酮|CsnPharm

CAS No.: 1431697-89-0

OTSSP167 Catalog No. CSN17846

Synonyms: OTS167;MELK Inhibitor

OTSSP167 is a potent MELK inhibitor with IC50 value of 0.41 nM, which block the phosphorylation of MELK-specific substrates.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MELK

IC50:0.41nM
描述OTSSP167 is a highly potent MELK inhibitor with IC50 of 0.41nM, exhibiting suppression of the growth of cancer stem cells. OTSSP167 at concentration of 10nM inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrinlike), two novel MELK substrates, in breast cancer cell lines. OTSSP167 suppressed the formation of mammosphere of MCF-7 cells in a dose-dependent manner at concentration ranging in 0.02-0.16μM. OTSSP167 exhibited anti-proliferative effect on A549 (lung), T47D (breast), DU4475 (breast), and 22Rv1 (prostate) cancer cells with IC50 values of 6.7, 4.3, 2.3, and 6.0 nM, respectively, but with much lower potency against cell line expressing MELK at low level, such as HT1197. Oral administration of OTSSP167 achieved tumor growth inhibition by 124% in mice carrying A549 (lung cancer) xenografts, 106% in mice carrying DU145 (prostate cancer) xenografts and 87% in mice carrying MIAPaCa-2 (pancreatic cancer) xenografts at dose of 10 mg/kg once a day.
作用机制OTSSP167 optimally occupies the active site of MELK, especially the hydrophobic back pocket, mainly through van der Waals interactions.^[2]
动物研究
剂量
Mice: 1 mg/kg - 20 mg/kg^[1] (i.v.); 5 mg/kg, 10mg/kg^[1] (p.o.）

给药途径
i.v., p.o.
参考文献

动物研究
剂量	Mice: 1 mg/kg - 20 mg/kg^[1] (i.v.); 5 mg/kg, 10mg/kg^[1] (p.o.）
给药途径	i.v., p.o.

[1] Chung S, Suzuki H, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012 Dec;3(12):1629-40.
[2] Cho YS, Kang Y, et al. The crystal structure of MPK38 in complex with OTSSP167, an orally administrative MELK selective inhibitor. Biochem Biophys Res Commun. 2014 Apr 25;447(1):7-11.

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
- 2.0516 mL
- 10.2581 mL
- 20.5161 mL
- 5 mM
- 0.4103 mL
- 2.0516 mL
- 4.1032 mL
- 10 mM
- 0.2052 mL
- 1.0258 mL
- 2.0516 mL

技术信息

CAS号

1431697-89-0

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

C25H28Cl2N4O2

运输

蓝冰

分子量

487.42

别名

OTS167;MELK Inhibitor

溶解度

DMSO	2.0 mg/mL (4.1 mM) warming
Water	insoluble
Ethanol	insoluble

动物实验配方

IP	2% DMSO+water	0.04 mg/mL	clear
PO	0.5% CMC-Na	31 mg/mL	suspension

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