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MELK-8a hydrochloride

Catalog No. T11996 CAS 2096992-20-8

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

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MELK-8a hydrochloride Chemical Structure

MELK-8a hydrochloride, CAS 2096992-20-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 147.00
5 mg	In stock	$ 347.00
10 mg	In stock	$ 497.00
25 mg	In stock	$ 793.00
50 mg	In stock	$ 1,130.00
100 mg	In stock	$ 1,520.00
500 mg	In stock	$ 2,970.00
1 mL * 10 mM (in DMSO)	In stock	$ 358.00

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Purity: 99.87%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Molecular Weight	469.02
Formula	C25H33ClN6O
CAS No.	2096992-20-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 100 mg/mL (213.21 mM)

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

References and Literature

1. Touré BB, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Ovarian Cancer Compound Library Bioactive Compounds Library Max Anti-Prostate Cancer Compound Library Anti-Obesity Compound Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Kinase Inhibitor Library Anti-Lung Cancer Compound Library Neuronal Differentiation Compound Library

Related Products

Related compounds with same targets

HTH-01-091 OTSSP167 MELK-IN-1 NMS-P715 MELK-8a Dihydrochloride JTV-519 hemifumarate Antitumor agent-116 OTSSP167 hydrochloride

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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.

Keywords

MELK-8a hydrochloride 2096992-20-8 PI3K/Akt/mTOR signaling MELK MELK-8a Hydrochloride MELK-8a inhibit NVS-MELK8a MELK8a hydrochloride Maternal embryonic leucine zipper kinase Inhibitor MELK 8a hydrochloride inhibitor

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