XY153 is is a BD2-selective BET inhibitor. XY153 potently bound to BRD4 BD2 with an half-maximum inhibitory concentration (IC50) value of 0.79 nM and displayed 354-fold selectivity over BRD4 BD1. Besides, XY153 exhibited 6-fold BRD4 BD2 domain selectivity over other BET BD2 domains. XY153 displayed potent antiproliferative activity against multiple tumor cell lines, especially MV4-11 (IC50 = 0.55 nM), while showing weak cytotoxicity against the normal lung fibroblast cell line. It highlights the safety profile of this series of BD2 inhibitors. 8l also demonstrated good metabolic stability in vitro.
MedKoo Cat#: 466103
Name: XY153
CAS#: unknown
Chemical Formula: C33H34FN3O4
Exact Mass: 555.2533
Molecular Weight: 555.65
Elemental Analysis: C, 71.33; H, 6.17; F, 3.42; N, 7.56; O, 11.52
The following data is based on the product molecular weight 555.65 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 |
