OTS-167 hydrochloride |CAS:1431698-10-0 Probechem Biochemicals

Chemical Structure : OTS-167 hydrochloride

CAS No.: 1431698-10-0

OTS-167 hydrochloride (OTSSP-167 hydrochloride)

Catalog No.: PC-44481Not For Human Use, Lab Use Only.

OTSSP167 hydrochloride (OTS-167) is a highly potent, selective and orally active MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.

Packing	Price	Stock
25 mg	$198	In stock
50 mg	$298	In stock
100 mg	$458	In stock
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1 g		Get quote

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Biological Activity

OTSSP167 hydrochloride (OTS-167) 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.

Physicochemical Properties

M.Wt	523.8824
Formula	C25H29Cl3N4O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 5.6 mg/mL; H2O: 2 mg/mL
Chemical Name/SMILES	1-(6-(3,5-dichloro-4-hydroxyphenyl)-4-(((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)amino)-1,5-naphthyridin-3-yl)ethanone hydrochloride

References

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.

OTS-167 hydrochloride (OTSSP-167 hydrochloride)

Biological Activity

Physicochemical Properties

References

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