1619994-68-1
1619994-68-1 结构式
基本信息
1-(1-(2-(甲磺酰)苯基)-7-丙氧基吲哚嗪-3-基)乙酮
1-[1-[2-(甲基磺酰基)苯基]-7-丙氧基-3-吲哚嗪基]乙酮
GSK2801
GSK 280
GSK 2801
GSK-2801
GSK2801, >98%
GSK-2801
GSK 280
GSK2801 GSK-2801
GSK2801
GSK-2801
GSK 2801
1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
物理化学性质
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/02/08 | HY-15658 | GSK2801 GSK2801 | 1619994-68-1 | 5mg | 623元 |
| 2025/02/08 | HY-15658 | GSK2801 GSK2801 | 1619994-68-1 | 10mM * 1mLin DMSO | 715元 |
| 2025/02/08 | HY-15658 | GSK2801 GSK2801 | 1619994-68-1 | 10mg | 870元 |
常见问题列表
Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B)
GSK2801 binds TAF1L(2) with an affinity K
B
of 0.31μM (K
D
: 3.2 μM) and a binding enthalpy change ΔH of −8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity K
B
of 0.826 μM (K
D
: 1.1 μM) and ΔH of −9.8 kcal/mol.
GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC.
In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.