IHMT-EZH2-115 is a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor (IC50 – 26 nM) for the Treatment of B-Cell Lymphomas. In the biochemical assay, IHMT-EZH2-115 inhibited EZH2 (IC50 = 26.1 nM) with high selectivity over other histone methyltransferases. It was also potent against EZH2 mutants (EZH2 Y641F, IC50 = 72.3 nM). Furthermore, it showed no apparent inhibitory activity against the human ether-á-go-go related gene (hERG) (IC50 > 30 μM). In vivo, IHMT-EZH2-115 exhibited favorable pharmacokinetic properties for oral administration and showed better efficacy than 1 in both Pfeiffer and Karpas-422 cell-mediated xenograft mouse models, indicating that it might be a new potential therapeutic candidate for EZH2 mutant cancers.
MedKoo Cat#: 465629
Name: IHMT-EZH2-115
CAS#: unknown
Chemical Formula: C36H46N6O3
Exact Mass: 610.3631
Molecular Weight: 610.80
Elemental Analysis: C, 70.79; H, 7.59; N, 13.76; O, 7.86
The following data is based on the product molecular weight 610.80 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 |
