HH2853 S-isomer is an S isomer of HH2853. HH-2853 is a potent EZH1/2 inhibitor with potent anti-tumor activities. HH2853 inhibited the enzymatic activities of wild-type and mutant EZH2 with IC50 values of 2.21-5.36 nM, which was similar to that of tazemetostat. In addition, HH2853 inhibited EZH1 enzymatic activity with an IC50 of 9.26 nM, which was stronger than tazemetostat (IC50: 58.43 nM). In contrast, HH2853 up to 10 μM exhibited only marginal or minor inhibitory activity against 36 histone modification enzymes. At cellular level, HH2853 potently inhibited H3K27 mono-, di- and tri-methylation in multiple cancer cell lines with wild-type or mutant EZH2. In contrast, HH2853 up to 10 μM had no effect on the other types of methylation modifications on histone H3. Moreover, HH2853 potently inhibited the cell viability of multiple cancer cell lines with EZH2 GOF mutation or alterations in SWI/SNF complex, and exhibited superior anti-tumor efficacy in several tumor xenograft models than tazemetostat at a comparable dose level. Furthermore, HH2853 exhibited superior PK property than tazemetostat.
MedKoo Cat#: 207206
Name: HH2853 S-isomer
CAS#: 2202678-05-3 (S-isomer)
Chemical Formula: C31H36F3N7O3
Exact Mass: 611.2832
Molecular Weight: 611.67
Elemental Analysis: C, 60.87; H, 5.93; F, 9.32; N, 16.03; O, 7.85
The following data is based on the product molecular weight 611.67 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 |
