OTSSP167HCL

ChemicalBook > CAS DataBase List > OTSSP167HCL

Product Name: OTSSP167HCL
CAS No.: 1431698-10-0
Chemical Name: OTSSP167HCL
Synonyms: OTS167 HCl;OTSSP167HCL;OTSSP167 HCl (OTS167);OTS-167 hydrochloride;OTSSP167 HCl (OTS167 HCl);MELK INHIBITOR; OTSSP-167; OTSSP 167;OTSSP167hydrochloride/OTSSP-167hydrochloride;1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone hydrochloride;Ethanone,1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-,hydrochloride(1:1);OTSSP-167,OTSSP 167,OTSSP167,OTSSP167 hydrochloride,MELK,OTSSP-167 hydrochloride,Maternal embryonic leucine zipper kinase,inhibit,OTS167,OTS-167,OTS 167,Inhibitor
CBNumber: CB52718395
Molecular Formula: C25H29Cl3N4O2
Formula Weight: 523.88236
MOL File: 1431698-10-0.mol

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OTSSP167HCL Property

storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: crystalline solid
color: Light yellow to gray

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Danger

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16873
Product name: OTSSP167 (hydrochloride)
Purity: ≥95%
Packaging: 1mg
Price: $62
Updated: 2024/03/01

Cayman Chemical

Product number: 16873
Product name: OTSSP167 (hydrochloride)
Purity: ≥95%
Packaging: 5mg
Price: $270
Updated: 2024/03/01

Cayman Chemical

Product number: 16873
Product name: OTSSP167 (hydrochloride)
Purity: ≥95%
Packaging: 10mg
Price: $477
Updated: 2024/03/01

ChemScene

Product number: CS-1241
Product name: OTSSP167(hydrochloride)
Purity: 99.84%
Packaging: 5mg
Price: $180
Updated: 2021/12/16

ApexBio Technology

Product number: B1308
Product name: OTSSP167hydrochloride
Packaging: 2mg
Price: $215
Updated: 2021/12/16

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OTSSP167HCL Chemical Properties,Usage,Production

Biological Activity

otssp167 is an inhibitor of maternal embryonic leucine zipper kinase(melk) with ic50 value of 0.41nm [1].melk belongs to the ampk serine/threonine kinase family and involves in the mammalian embryonic development. it overexpresses in various types of human cancer. otssp167 is synthetized from a compound which is a hit of a high-throughput screening. in vitro anti-proliferative assay shows that otssp167 suppresses cell growth of various cancer cell lines, such as a549(ic50=6.7nm), t47d(ic50=4.3nm), du4475(ic50=2.3nm) and 22rv1(ic50= 6.0nm). in vivo assay also shows otssp167 can significantly suppress tumor growth in the xenograft model using various cancer cell lines. the effects are observed by both intravenous administration and oral administration. when investigating the substrates of melk, otssp167 is found to inhibit the phosphorylation of dbnl and psma1 in vitro. since psma1 is essential for survival of cancer cells, the reduction of phosphorylated psma1 caused by otssp167 can subsequently suppress mammosphere formation of cancer stem cells [1].

in vitro

OTSSP167 inhibits the growth of A549 (lung), T47D (breast), DU4475 (breast), 22Rv1 (prostate) and HT1197 (bladder) cancer cells with IC ₅₀ values of 6.7 , 4.3, 2.3, 6.0 and 97 nM, respectively. It can abrogate the mitotic checkpoint, disrupt MCC and MCC-APC/C interaction in MCF7 cells, and causes GFP-MELK localization to cell cortex in prometaphase cells. OTSSP167 is a MELK selective inhibitor, exhibits a strong in vitro activity, conferring an IC ₅₀ of 0.41 nM.

in vivo

OTSSP167 (20 mg/kg, iv) results in tumor growth inhibition (TGI) of 73% in xenograft mouse model; OTSSP167 (1, 5, and 10 mg/kg, po) reveals TGI of 51, 91, and 108%, respectively. OTSSP167 (20 mg/kg, po) shows no tumor growth suppressive effect on PC-14 xenografts.

target

IC50: 0.41 nM (MELK)

References

[1] suyoun chung, hanae suzuki, takashi miyamoto et al. development of an orally-administrative melk-targeting inhibitor that suppresses the growth of various types of human cancer. oncotarget. 2012, 3: 1629-1640.

OTSSP167HCL Preparation Products And Raw materials

Raw materials

Preparation Products

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1431698-10-0, OTSSP167HCLRelated Search:

Pyridine hydrochloride SULFAPHENAZOLE Aniline hydrochloride Trimethylamine hydrochloride Betaine hydrochloride Methylamine hydrochloride Dimethylamine hydrochloride

OTSSP167HCL

OTSSP167hydrochloride/OTSSP-167hydrochloride

OTSSP167 HCl (OTS167 HCl)

1-[6-(3,5-Dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-ethanone hydrochloride

MELK INHIBITOR; OTSSP-167; OTSSP 167

OTS-167 hydrochloride

Ethanone,1-[6-(3,5-dichloro-4-hydroxyphenyl)-4-[[trans-4-[(dimethylamino)methyl]cyclohexyl]amino]-1,5-naphthyridin-3-yl]-,hydrochloride(1:1)

OTSSP167 HCl (OTS167)

OTSSP-167,OTSSP 167,OTSSP167,OTSSP167 hydrochloride,MELK,OTSSP-167 hydrochloride,Maternal embryonic leucine zipper kinase,inhibit,OTS167,OTS-167,OTS 167,Inhibitor

OTS167 HCl

1431698-10-0

C25H28Cl2N4O2HCl

C25H29Cl3N4O2