SKLB-03220 is a covalent EZH2 Inhibitor (IC50 = 1.72 nM) Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer. SKLB-03220 could covalently bind to the S-adenosylmethionine (SAM) pocket of EZH2. Besides, SKLB-03220 was highly potent for EZH2MUT, while exhibiting weak activities against other tested histone methyltransferases (HMTs) and kinases. Moreover, SKLB-03220 displayed noteworthy potency against ovarian cancer cell lines and continuously abolished H3K27me3 after washing out. Furthermore, oral administration of SKLB-03220 significantly inhibited tumor growth in PA-1 xenograft model without obvious adverse effects.
MedKoo Cat#: 122621
Name: SKLB-03220
CAS#: N/A
Chemical Formula: C33H40N4O4
Exact Mass: 556.3000
Molecular Weight: 556.71
Elemental Analysis: C, 71.20; H, 7.24; N, 10.06; O, 11.50
The following data is based on the product molecular weight 556.71 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 |
