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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-MELK-OTS167
OTS167

Chemical Structure : OTS167

CAS No.: 1431697-89-0

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OTS167 (OTSSP167, OTS-167)

货号: PC-44480Not For Human Use, Lab Use Only.

OTSSP167 (OTS167) is a highly potent, selective and orally active MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

OTSSP167 (OTS167) is a highly potent, selective and orally active MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
OTSSP167 demonsrates in vitro anti-proliferative against MELK-highly expressed A549 (lung), T47D (breast), DU4475 (breast), and 22Rv1 (prostate) cancer cells with IC50 of 6.7, 4.3, 2.3, and 6.0 nM, respectively, with significant lower activity against HT1197 (bladder, low-MELK expression) cancer cells (IC50=97 nM).
OTSSP167 shows the effectiveness on the growth of various human cancer xenograft.
OTSSP167 inhibits the phosphorylation of novel MELK substrates, significantly suppresses the phosphorylation levels of DBNL and PSMA1 in breast cancer cell lines.

物理化学性质&存储条件

分子量 487.4214
分子式 C25H28Cl2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(6-(3,5-dichloro-4-hydroxyphenyl)-4-(((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)amino)-1,5-naphthyridin-3-yl)ethanone

参考文献

1. Chung S, et al. Oncotarget. 2012 Dec;3(12):1629-40.

2. Alachkar H, et al. Oncotarget. 2014 Dec 15;5(23):12371-82.

3. Stefka AT, et al. Blood Cancer J. 2016 Aug 19;6(8):e460.

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