A potent inhibitor of MELK (IC50 = 0.41 nM); blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel; suppresses the growth of xenograft tumors in mice

OTSSP167 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1431698-10-0
Storage:
-20
UN-No:
Non-Hazardous - /

Maternal embryonic leucine zipper kinase (MELK) is a serine/threonine kinase that regulates signaling central to cell cycling, stem cell renewal, apoptosis, and other cellular processes.{27684} MELK is overexpressed in some forms of cancer, particularly those with aggressive undifferentiated tumors.{27683,24926,24930} OTSSP167 is a potent inhibitor of MELK (IC50 = 0.41 nM).{27685} It suppresses the growth of diverse cancer cell lines at low nanomolar concentrations.{27685} It also blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel.{27685} OTSSP167 is also effective in vivo when delivered either orally or intravenously, suppressing the growth of xenograft tumors in mice.{27685,27686}  

 

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Description

A potent inhibitor of MELK (IC50 = 0.41 nM); blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel; suppresses the growth of xenograft tumors in mice

Formal name: 1-(6-(3,5-dichloro-4-hydroxyphenyl)-4-(((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)amino)-1,5-naphthyridin-3-yl)ethan-1-one, monohydrochloride

Synonyms: 

Molecular weight: 523.9

CAS: 1431698-10-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling

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