YM181 is a proteolysis-target chimera (PROTAC)-based EZH2 degrader. YM181 induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degrader displayed promising antitumor activities in lymphoma xenografts and patient-derived primary. lymphoma cells. The study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.
MedKoo Cat#: 464923
Name: YM181
CAS#: unknown
Chemical Formula: C57H73N7O10S
Exact Mass: 1047.5140
Molecular Weight: 1048.31
Elemental Analysis: C, 65.31; H, 7.02; N, 9.35; O, 15.26; S, 3.06
The following data is based on the product molecular weight 1,048.31 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 |
