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MELK-8a hydrochloride

Name: MELK-8a hydrochloride
Brand: TargetMol
SKU: T11996
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T11996Cas No. 2096992-20-8

MELK-8a hydrochloride is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK, IC50 = 2 nM).

MELK-8a hydrochloride

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Purity: 99.87%

Catalog No. T11996Cas No. 2096992-20-8

MELK-8a hydrochloride is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK, IC50 = 2 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$48	In Stock	In Stock
10 mg	$77	In Stock	In Stock
25 mg	$158	In Stock	In Stock
50 mg	$251	In Stock	In Stock
100 mg	$371	In Stock	In Stock
200 mg	$517	-	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.87%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	MELK-8a hydrochloride is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK, IC50 = 2 nM).
Targets&IC50	MELK:2 nM
In vitro	MELK-8a hydrochloride inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2 μM, respectively. MELK-8a hydrochloride remains very potent with an IC50 of 140 nM when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. MELK-8a hydrochloride only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. MELK-8a hydrochloride is at least 90-fold more selective in targeting MELK in all cases. MELK-8a hydrochloride is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay[1].
In vivo	In C57BL/6 mice, MELK-8a hydrochloride (30 mg/kg; s.c.) results in good plasma exposure. The compound adsorption into the systemic circulation is rapid (Tmax=0.4 h) and peak plasma concentration reaches 6.6 μM. An ascending dose PK study in female athymic nude mice shows that the rate of compound release is maximal at 120 mg/kg and all clearance mechanisms can be saturated at 240 mg/kg. However, MELK-8a hydrochloride (10 mg/kg; oral) shows very poor PK (3.6% oral bioavailability) consistent with very high in vivo clearance[1].

Chemical Properties

Molecular Weight	469.02
Formula	C₂₅H₃₃ClN₆O
Cas No.	2096992-20-8
Smiles	Cl.CN1CCN(CC1)c1ccc(cc1)-n1cc(cn1)-c1ccncc1OCC1CCNCC1
Relative Density.	1.31g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 100 mg/mL (213.21 mM), Sonication is recommended.

DMSO: 8 mg/mL (17.06 mM), Sonication and heating are recommended.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.1321 mL	10.6605 mL	21.3211 mL	106.6053 mL
5 mM	0.4264 mL	2.1321 mL	4.2642 mL	21.3211 mL
10 mM	0.2132 mL	1.0661 mL	2.1321 mL	10.6605 mL

H2O

	1mg	5mg	10mg	50mg
20 mM	0.1066 mL	0.5330 mL	1.0661 mL	5.3303 mL
50 mM	0.0426 mL	0.2132 mL	0.4264 mL	2.1321 mL
100 mM	0.0213 mL	0.1066 mL	0.2132 mL	1.0661 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc