| Identification | Back Directory | [Name]
OTSSP 167 hydrochloride | [CAS]
1431697-89-0 | [Synonyms]
OTS167
CS-1147
CS-1832
OTSSP167
OTSSP-167
OTSSP 167
MELK inhibitor
OTSSP167 (CS-1147)
OTSSP167 (Free base)
OTSSP 167 hydrochloride
OTSSP-167 hydrochloride
OTSSP167 (hydrochloride)
1-(8-((1R,4R)-4-((Dimethylamino)methyl)cyclohexylamino)-2-(3,5-dichloro-4-hydroxyphenyl)-1,5-naphthyridin-7-yl)ethanone
1-(6-(3,5-dichloro-4-hydroxyphenyl)-4-((1r,4r)-4-((dimethylamino)methyl)cyclohexylamino)-1,5-naphthyridin-3-yl)ethanone
1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone
Ethanone, 1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-
1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone OTSSP167 hcl | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C25H28Cl2N4O2 | [MDL Number]
MFCD23160047 | [MOL File]
1431697-89-0.mol | [Molecular Weight]
487.42 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor. | [Definition]
ChEBI: 4-[7-acetyl-8-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1H-1,5-naphthyridin-2-ylidene]-2,6-dichloro-1-cyclohexa-2,5-dienone is a naphthyridine derivative. | [Biological Activity]
otssp167 is an inhibitor of maternal embryonic leucine zipper kinase (melk) with ic50 value of 0.41nm [1].melk is a member of the ampk serine/threonine kinase family and is involved in the mammalian embryonic development. it plays roles in cancer cell growth and formation or maintenance of cancer stem cells. otssp167 is a small-molecule inhibitor and can inhibit melk’s activity effectively and selectively. otssp167 inhibits cell proliferation of a variety of cancer cell lines including a549, t47d, du4475 and 22rv1. the ic50 values are 6.7nm, 4.3nm, 2.3nm and 6nm, respectively. in mice bearing mda-mb-231 xenograft, administration of otssp167 inhibits 70% tumor growth at dose of 20 mg/kg. besides that, otssp167 is also found to have effects on psma1 and dbnl which are the novel substrates of melk. it inhibits the phosphorylation of psma1 and dbnl causes the subsequent suppression of mammosphere formation [1]. | [in vivo]
OTSSP167 (20 mg/kg, i.v.) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, p.o.) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, p.o.) shows no tumor growth suppressive effect on PC-14 xenografts[1]. | [target]
MELK | [storage]
Store at -20°C | [References]
[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, 3(12): 1629. |
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| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Twochem Co.Ltd
|
| Telephone: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
|