1395347-24-6
|
|
- CAS号:
- 1395347-24-6
- 英文名:
- ISA-2011B
- 英文别名:
- ISA-2011B;ISA2011B; ISA 2011B;ISA-2011B,Inhibitor,inhibit,ISA 2011B,ISA2011B;5H-1,3-Dioxolo[4,5-g]pyrazino[1,2-b]isoquinoline-7,10-dione, 5-(5-chloro-1H-indol-3-yl)-8,9,10a,11-tetrahydro-9-methyl-, (5S,10aS)-
- 中文名:
- 1395347-24-6
- 中文别名:
- 化合物 T15597;化合物ISA-2011B;PIP5KΑ抑制剂(ISA-2011B)
- CBNumber:
- CB23167641
- 分子式:
- C22H18ClN3O4
- 分子量:
- 423.85
- MOL File:
- 1395347-24-6.mol
|
|
|
1395347-24-6化学性质
-
沸点:
-
714.9±60.0 °C(Predicted)
-
|
-
密度:
-
1.58±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
DMSO:100.0(Max Conc. mg/mL);235.93(Max Conc. mM)
-
|
-
酸度系数(pKa):
-
15.58±0.30(Predicted)
-
|
1395347-24-6性质、用途与生产工艺
ISA-2011B是PIP5K1α的抑制剂, 具有抗癌活性。
The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is significantly reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively. ISA-2011B exhibits the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells. ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR.
ISA-2011B significantly inhibits growth of tumor cells in xenograft mice, and is mediated by targeting PIP5K1α-associated PI3K/AKT and the downstream survival, proliferation, and invasion pathways. Overexpression of AR-V7 increases PIP5K1α, promotes rapid growth of PCa in xenograft mice, whereas inhibition of PIP5K1α by its inhibitor ISA-2011B suppresses the growth and invasiveness of xenograft tumors overexpressing AR-V7. ISA-2011B disrupts protein stabilization of AR-V7 which is dependent on PIP5K1α, leading to suppression of invasive growth of AR-V7-high tumors in xenograft mice.
1395347-24-6
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-16937 | 1395347-24-6 ISA-2011B | 1395347-24-6 | 1mg | 1100元 |
2024/04/30 | HY-16937 | 1395347-24-6 ISA-2011B | 1395347-24-6 | 5mg | 2400元 |
1395347-24-6, 1395347-24-6 相关搜索:
- 细胞生物学试剂
- 化合物ISA-2011B
- 化合物 T15597
- PIP5KΑ抑制剂(ISA-2011B)
- 1395347-24-6
- ISA-2011B,Inhibitor,inhibit,ISA 2011B,ISA2011B
- 5H-1,3-Dioxolo[4,5-g]pyrazino[1,2-b]isoquinoline-7,10-dione, 5-(5-chloro-1H-indol-3-yl)-8,9,10a,11-tetrahydro-9-methyl-, (5S,10aS)-
- ISA2011B; ISA 2011B
- ISA-2011B