EPZ031686
- CAS No.
- 1808011-22-4
- Chemical Name:
- EPZ031686
- Synonyms
- CS-2707;EPZ031686;EPZ031686;EPZ-031686;EPZ 031686;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
- CBNumber:
- CB43126530
- Molecular Formula:
- C26H34ClF3N4O4S
- Molecular Weight:
- 0
- MDL Number:
- MFCD30181978
- MOL File:
- Mol file
EPZ031686 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ApexBio Technology | B6082 | EPZ031686 | 1808011-22-4 | 1mg | $150 | 2021-12-16 | Buy |
| ChemScene | CS-5775 | EPZ031686 99.82% | 1808011-22-4 | 1mg | $180 | 2021-12-16 | Buy |
| ApexBio Technology | B6082 | EPZ031686 | 1808011-22-4 | 5mg | $350 | 2021-12-16 | Buy |
| ChemScene | CS-5775 | EPZ031686 99.82% | 1808011-22-4 | 5mg | $420 | 2021-12-16 | Buy |
| ChemScene | CS-5775 | EPZ031686 99.82% | 1808011-22-4 | 10mg | $600 | 2021-12-16 | Buy |
EPZ031686 Chemical Properties,Uses,Production
Biological Activity
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].
IC 50
3 nm
References
[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.
EPZ031686 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32951 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29811 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38596 | 58 | |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 | Mandy@hangyubiotech.com | China | 10986 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
| Shanghai Changyu Medical Technology Co. Ltd. | +86-13301875428 | sales@changyuhe.com | China | 305 | 58 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7552 | 61 |
