S84032 |
EPZ031686 |
| 源叶(MedMol) | 99% |
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- 产品描述： EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.
- 靶点： Histone Methyltransferase
- 体内研究： 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.
- 参考文献：
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.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.692 ml 8.459 ml 16.918 ml 5 mM 0.338 ml 1.692 ml 3.384 ml 10 mM 0.169 ml 0.846 ml 1.692 ml 50 mM 0.034 ml 0.169 ml 0.338 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
