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OTSSP167

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Chemical Structure| 1431697-89-0 同义名 : OTS167
CAS号 : 1431697-89-0
货号 : A158718
分子式 : C25H28Cl2N4O2
纯度 : 99%+
分子量 : 487.421
MDL号 : MFCD23160047
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: 2 mg/mL(4.1 mM)，配合低频超声，水浴加热至45℃，并调节pH至4，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：

IP 2% DMSO+water 0.04 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

生物活性
靶点

  • MELK

    MELK, IC50:0.41 nM
描述 OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC50 values of 6.7, 4.3, 2.3, 6.0 and 97 nM, respectively[1]. OTSSP167 effectively interferes with the mitotic checkpoint and disrupts MCC and MCC-APC/C interactions in MCF7 cells, also causing GFP-MELK localization to the cell cortex in prometaphase cells[2]. As a selective MELK inhibitor, OTSSP167 exhibits a strong in vitro activity with an IC50 of 0.41 nM[3].
作用机制 OTSSP167 optimally occupies the active site of MELK, especially the hydrophobic back pocket, mainly through van der Waals interactions.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.26mL

2.05mL

1.03mL

20.52mL

4.10mL

2.05mL
参考文献

[1]Chung S, Suzuki H, Miyamoto T, et al. Development of an orally-administrative MELK-targeting inhibitor that suppresses the growth of various types of human cancer. Oncotarget. 2012 Dec 21.

[2]Li S, et al. Maternal embryonic leucine zipper kinase serves as a poor prognosis marker and therapeutic target in gastric cancer. Oncotarget. 2016 Feb 2;7(5):6266-80.

[3]Ji W, et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases. PLoS One. 2016 Apr 15;11(4):e0153518.