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EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $113 | In Stock | |
5 mg | $263 | In Stock | |
10 mg | $396 | In Stock | |
25 mg | $788 | In Stock | |
50 mg | $1,130 | In Stock | |
100 mg | $1,520 | In Stock | |
1 mL x 10 mM (in DMSO) | $359 | In Stock |
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]. |
Alias | EPZ-031686 |
Molecular Weight | 591.09 |
Formula | C26H34ClF3N4O4S |
Cas No. | 1808011-22-4 |
Smiles | FC(F)(F)CCCN1CCC(CS(=O)(=O)N2[C@H]3CC[C@@H]2C[C@@H](C3)NC(=O)c2cc3CC(=O)Nc3cc2Cl)CC1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (50.8 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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