GSK2801
|
|
|
- CAS號:
- 1619994-68-1
- 英文名:
- GSK 2801
- 英文別名:
- GSK 280;CS-1607;GSK2801;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
- 中文名:
- GSK2801
- 中文別名:
- 化合物GSK2801;GSK2801,BAZ2A和BAZ2B抑制劑;BAZ2A和BAZ2B抑制劑(GSK2801);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?；?苯基]-7-丙氧基-3-吲哚嗪基]乙酮
- CBNumber:
- CB52668513
- 分子式:
- C20H21NO4S
- 分子量:
- 371.45
- MOL File:
- 1619994-68-1.mol
|
|
|
GSK2801化學性質
-
密度:
-
1.23±0.1 g/cm3(Predicted)
-
|
-
儲存條件:
-
-20°C
-
|
-
溶解度:
-
insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥2.82 mg/mL in EtOH with gentle warming and ultrasonic
-
|
-
形態(tài):
-
solid
-
|
-
顏色:
-
Light yellow to khaki
-
|
GSK2801性質、用途與生產工藝
GSK2801 是一種有效的，選擇性的，口服活性的和細胞活性的乙酰賴氨酸競爭性 BAZ2A 和 BAZ2B 溴結構域抑制劑，Kd 值分別為 136 nM 和 257 nM。GSK2801 對 BAZ2A/B 的選擇性是 BRD4 的 50 倍以上。
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.
GSK2801
上下游產品信息
上游原料
下游產品
| 更新日期 | 產品編號 | 產品名稱 | CAS編號 | 包裝 | 價格 |
|---|
| 2024/11/08 | 46803 | GSK2801, 95%
GSK2801, 95% | 1619994-68-1 | 100mg | 9718元 |
| 2024/11/08 | HY-15658 | GSK2801
GSK2801 | 1619994-68-1 | 5mg | 623元 |
1619994-68-1, GSK2801 相關搜索:
- Inhibitors
- 抑制劑
- 合成有機化合物配體
- 細胞生物學試劑
- 小分子抑制劑，天然產物
- 小分子抑制劑
- GSK2801,BAZ2A和BAZ2B抑制劑
- 化合物GSK2801
- 1-(1-(2-(甲磺酰)苯基)-7-丙氧基吲哚嗪-3-基)乙酮
- BAZ2A和BAZ2B抑制劑(GSK2801)
- 1-[1-[2-(甲基磺?；?苯基]-7-丙氧基-3-吲哚嗪基]乙酮
- 1619994-68-1
- inhibit,Inhibitor,GSK-2801,TNBC,BAZ2A,GSK2801,Epigenetic Reader Domain,Apoptosis,BAZ2B,cetyl-lysine,orally,GSK 2801
- GSK2801 GSK-2801
- 1-[1-(2-Methanesulfonyl-phenyl)-7-propoxy-indolizin-3-yl]-ethanone
- GSK2801;GSK-2801;GSK 2801
- CS-1607
- GSK2801, >98%
- GSK 280
- GSK-2801; GSK 280
- Ethanone, 1-[1-[2-(methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]-
- 1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
- 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone
- 1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone
- GSK-2801
- GSK2801
- GSK 2801