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EPZ020411 2HCl (1700663-41-7(free base))

Catalog No. T4334 CAS T4334

EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).

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EPZ020411 2HCl (1700663-41-7(free base)) Chemical Structure

EPZ020411 2HCl (1700663-41-7(free base)), CAS T4334

Pack Size	Availability	Price/USD
2 mg	Inquiry	$ 108.00
5 mg	Inquiry	$ 192.00
10 mg	Inquiry	$ 306.00
25 mg	Inquiry	$ 639.00
1 mL * 10 mM (in DMSO)	Inquiry	$ 306.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
Targets&IC50	PRMT8:223 nM, PRMT1:119 nM, PRMT6:10 nM
In vitro	In A375 human melanoma cells exogenously overexpressing PRMT6,treatment with EPZ020411IC50=0.637±0.241 μM) results in a dose-dependent decrease in H3R2 methylation.
In vivo	Male Sprague-Dawley rats administered a single dose of EPZ020411 (1 mg/kg by i.v.) ,show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. At dose of EPZ020411(5 mg/kg s.c.) a good bioavailability of 65.6 ± 4.3% is observed, resulting on EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h.
Cell Research	A375 (CRL-1619) cells are incubated in the presence of increasing concentrations of EPZ020411 up to 20 μM for 48 hours.
Animal Research	Sprague-Dawley rats are treated with EPZ020411(1 mg/kg i.v.) prepared in saline, pH 6.5.

Molecular Weight	515.51
Formula	C25H40Cl2N4O3
CAS No.	T4334

Storage

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

Solubility Information

Ethanol: 93 mg/mL (180.4 mM)

DMSO: 93 mg/mL (180.4 mM)

References and Literature

1. Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659.

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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

EPZ020411 2HCl (1700663-41-7(free base)) T4334 Chromatin/Epigenetic Histone Methyltransferase EPZ020411 2HCl (1700663417(free base)) EPZ020411 2HCl (1700663 41 7(free base)) EPZ-020411 2HCl (1700663-41-7(free base)) inhibitor inhibit

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