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EPZ031686

Catalog No. TQ0263 CAS 1808011-22-4

Synonyms: EPZ-031686

EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

EPZ031686, CAS 1808011-22-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 147.00
2 mg	In stock	$ 213.00
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
1 mL * 10 mM (in DMSO)	In stock	$ 452.00

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Purity: 97.91%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.
Targets&IC50	SMYD3:3 nM (cell free)
In vivo	In male CD-1 mice, EPZ031686 (1 mg/kg; i.v.) shows a moderate clearance (CL) of 27 ± 3.9 mL/min/kg, in very good agreement with the mouse microsomal data, with a volume of distribution at steady state (Vss) of 2.3 ± 0.29 L/kg, translating to a mean terminal half-life (t1/2) of 1.7 ± 0.13 h. After the treatment of EPZ031686 (5 and 50 mg/kg; p.o.), both Cmax and AUC0‑last increased in a slightly higher than dose-proportional manner, while t1/2 remained unchanged. Bioavailability (F) of 48 ± 5.4% and 69 ± 8.2%, respectively, leading to EPZ031686 unbound blood concentration remaining above the SMYD3 ICW IC50 value for more than 12 h after a 50 mg/kg p.o.[1].

Synonyms	EPZ-031686
Molecular Weight	591.09
Formula	C26H34ClF3N4O4S
CAS No.	1808011-22-4

Storage

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

Solubility Information

DMSO: 30 mg/mL (50.8 mM), Sonication and heating to 60℃ are recommended.

References and Literature

1. Mitchell LH et al. Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Epigenetics Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library Histone Modification Compound Library

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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

EPZ031686 1808011-22-4 Chromatin/Epigenetic Histone Methyltransferase EPZ 031686 EPZ-031686 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.