- EPZ031686
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- $6.68 / 1KG
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2020-01-13
- CAS:1808011-22-4
- Min. Order: 1KG
- Purity: 97%-99%
- Supply Ability: 1kg-1000kg
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| | EPZ031686 Basic information |
| Product Name: | EPZ031686 | | Synonyms: | EPZ031686;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;EPZ031686;EPZ-031686;EPZ 031686;CS-2707 | | CAS: | 1808011-22-4 | | MF: | C26H34ClF3N4O4S | | MW: | 0 | | EINECS: | | | Product Categories: | | | Mol File: | Mol File | ![EPZ031686 Structure]() |
| | EPZ031686 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | insoluble in H2O; insoluble in EtOH; ≥104.6 mg/mL in DMSO |
| | EPZ031686 Usage And Synthesis |
| 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 |
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