Home PI3K/Akt/mTOR MELK inhibitor OTSSP167 For research use only.

OTSSP167

Synonyms: OTS167

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

OTSSP167 Chemical Structure

OTSSP167 Chemical Structure

CAS No. 1431697-89-0

Purity & Quality Control

OTSSP167 Related Products

Biological Activity

Description OTSSP167 (OTS167) is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
Features MELK-selective inhibitor.
Targets
MELK [1]
(Cell-free assay)
0.41 nM
In vitro
In vitro OTSSP167 inhibits A549, T47D, DU4475, and 22Rv1 cancer cells, in which MELK is highly expressed, with IC50 values of 6.7, 4.3, 2.3, and 6.0 nM, respectively. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which are novel MELK substrates and are important for stem-cell characteristics and invasiveness. OTSSP167 suppresses mammosphere formation of breast cancer cells through the inhibition of PSMA1 phosphorylation. [1]
Kinase Assay in vitro kinase assay
MELK recombinant protein (0.4 μg) is mixed with 5 μg of each substrate in 20 μL of kinase buffer containing 30 mM Tris-HCl (pH), 10 mM DTT, 40 mM NaF, 10 mM MgCl2, 0.1 mM EGTA with 50 μM cold-ATP and 10 Ci of [γ-32P]ATP for 30 min at 30 °C. The reaction is terminated by addition of SDS sample buffer and boiled for 5 min prior to SDS-PAGE. The gel is dried and autoradiographed with intensifying screens at room temperature. OTSSP167 (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation.
Cell Research Cell lines A549, T47D, DU4475, and 22Rv1, HT1197
Concentrations 0.005-0.1 μM
Incubation Time 72 h
Method Cell Counting Kit-8
In Vivo
In vivo OTSSP167 exhibits significant tumor growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. In MDA-MB-231 model, intravenous administration of OTSSP167 at 20 mg/kg once every two days results in TGI of 73% The oral administration at 10 mg/kg once a day reveals TGI of 72%. OTSSP167 for multiple cancer types in dose-dependent and MELK-dependent manners with no or a little body-weight loss. [1]
Animal Research Animal Models MDA-MB-231, A549, DU145 xenografts
Dosages 1 mg/kg , 5mg/kg ,10 mg/kg, 20 mg/kg
Administration oral

Chemical Information & Solubility

Molecular Weight 487.42 Formula

C25H28Cl2N4O2
CAS No. 1431697-89-0 SDF Download OTSSP167 SDF
Smiles CC(=O)C1=CN=C2C=CC(=NC2=C1NC3CCC(CC3)CN(C)C)C4=CC(=C(C(=C4)Cl)O)Cl
Storage (From the date of receipt)

In vitro
Batch:

4-Methylpyridine : 10 mg/mL

DMSO : 0.5 mg/mL ( (1.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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