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EPZ031686

Catalog No.GC16224

EPZ031686 est un inhibiteur SMYD3 puissant et actif par voie orale et avec une valeur IC50 de 3 nM. EPZ031686 peut être utilisé pour la recherche sur le cancer.

Products are for research use only. Not for human use. We do not sell to patients.

EPZ031686 Chemical Structure

Cas No.: 1808011-22-4

Taille Prix Stock Qté
1mg
102,00 $US
En stock
5mg
254,00 $US
En stock
10mg
337,00 $US
En stock
50mg
1 011,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 3 nM

EPZ031686 is the first SMYD3 inhibitor.

Set and Mynd Domain containing 3 (SMYD3), a lysine methyltransferase (KMT) expressed at high levels in a number of different cancer histologies, is reported to be associated with a poor clinical prognosis.

In vitro: EPZ031686 was the first SMYD3 inhibitor found to show double-digit nanomolar cellular activity. In addition, EPZ031686 displayed noncompetitive inhibition to both SAM and MEKK2 with a Ki = 1.2 and 1.1 nM, respectively. Moreover, EPZ031686 showed less than 30% inhibition against 16 histone methyltransferase targets at a 10 μM [1].

In vivo: Male mice i.v. administered a single dose of EPZ031686 at 1 mg/kg showed a moderate clearance of 27 mL/min/kg, which was in very good agreement with the microsomal data, with a volume of distribution at steady state of 2.3 L/kg, translating to a terminal half-life of 1.7 h. Around 20% of the administered dose was excreted unchanged in urine after 24 h, equivalent to a renal clearance of 5.3 mL/min/kg. Bioavailability of 48 and 69 was observed at 5 and 50 mg/kg, respectively, resulting in the EPZ031686 unbound blood concentration remaining above the SMYD3 IC50 value for more than 12 h after a 50 mg/kg p.o. administration [1].

Clinical trial: Up to now, EPZ031686 is still in the preclinical development stage.

Reference:
[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.

Chemical Properties

Cas No. 1808011-22-4 SDF
Chemical Name 6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluorobutyl)piperidin-4-yl)methyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
Canonical SMILES ClC1=CC(N2)=C(CC2=O)C=C1C(N[C@@]3([H])C[C@@](N4S(CC(CC5)CCN5CCCC(F)(F)F)(=O)=O)([H])CC[C@@]4([H])C3)=O
Formula C26H34ClF3N4O4S M.Wt 591.09
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.6918 mL 8.4589 mL 16.9179 mL
5 mM 0.3384 mL 1.6918 mL 3.3836 mL
10 mM 0.1692 mL 0.8459 mL 1.6918 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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