2231747-03-6
2231747-03-6 结构式
物理化学性质
沸点550.4±50.0 °C(Predicted)
密度1.273±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: ≥ 250 mg/mL (843.68 mM)
酸度系数(pKa)9.09±0.10(Predicted)
形态Solid
颜色White to off-white
常见问题列表
生物活性
OXFBD04 是一种有效的选择性 BRD4 抑制剂，IC50 为 166 nM。OXFBD04 是一种有效的 BET 溴结构域配体，对 CREBBP 溴结构域具有额外的适度亲和力。OXFBD04 具有抗癌活性。靶点
|
BRD4 166 nM (IC 50 ) |
体外研究
OXFBD04 (0.01-100 μM; 48 hours) inhibits cancer cell lines growth.
OXFBD04 (10 µM; for 10, 24, or 48 hours) induces MYC suppression in MCF7 breast cancer cells.
Cell Viability Assay
| Cell Line: | A498 (renal), HT-29 (colon), and MCF7 (breast) cancer cell lines |
| Concentration: | 0.01, 0.1, 1, 10, 100 μM |
| Incubation Time: | 48 hours |
| Result: | Inhibited cancer cell lines growth. |
体内研究
OXFBD04 has optimised physicochemical properties (LE=0.43; LLE=5.74; SFI=5.96), and good metabolic stability (t
1/2
=388 min). OXFBD04 has CL
int
of 3.57 µL/min/mg.