Name: OTSSP167
Brand: Selleck Chemicals
SKU: S7159
Rating: 5 (17 reviews)

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Quality Control

Batch: Purity: 99.47%

99.47

Related Targets	PI3K Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A
Other MELK Inhibitors	MELK-8a Dihydrochloride

Chemical Information, Storage & Stability

Molecular Weight	487.42	Formula	C₂₅H₂₈Cl₂N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1431697-89-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	OTS167			Smiles	CC(=O)C1=CN=C2C=CC(=NC2=C1NC3CCC(CC3)CN(C)C)C4=CC(=C(C(=C4)Cl)O)Cl

Solubility

In vitro
Batch:

4-Methylpyridine : 10 mg/mL

DMSO : 0.5 mg/mL (1.02 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
	5%4-Methylpyridine 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.05mM)
	5%4-Methylpyridine 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.05mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	MELK-selective inhibitor.
Targets/IC₅₀/Ki	MELK (Cell-free assay) 0.41 nM
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. This compound 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. It suppresses mammosphere formation of breast cancer cells through the inhibition of PSMA1 phosphorylation.
Kinase Assay	in vitro kinase assay
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. This compound (final concentration of 10 nM) is dissolved in DMSO and added to kinase buffer before the incubation.
In vivo	OTSSP167 exhibits significant tumour growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. In the MDA-MB-231 model, intravenous administration of this compound at 20 mg/kg once every two days results in TGI of 73%. Oral administration at 10 mg/kg once a day reveals TGI of 72%. This chemical acts for multiple cancer types in dose-dependent and MELK-dependent manners with no or little body-weight loss.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23283305/

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OTSSP167 MELK inhibitor

Chemical Structure

Molecular Weight: 487.42