EPZ-719 is a novel and potent SETD2 inhibitor (IC50=5 nM) with a high selectivity over other histone methyltransferases. A screening campaign of the Epizyme proprietary histone methyltransferase-biased library identified potential leads based on a 2-amidoindole core. Structure-based drug design (SBDD) and drug metabolism/pharmacokinetics (DMPK) optimization resulted in EPZ-719, an attractive tool compound for the interrogation of SETD2 biology that enables in vivo target validation studies.
MedKoo Cat#: 465415
Name: EPZ-719 HCl
CAS#: EPZ-719 HCl
Chemical Formula: C22H32ClFN4O3S
Exact Mass: 0.0000
Molecular Weight: 487.03
Elemental Analysis: C, 54.26; H, 6.62; Cl, 7.28; F, 3.90; N, 11.50; O, 9.86; S, 6.58
The following data is based on the product molecular weight 487.03 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
