COMPOUND 401
|
|
- CAS号:
- 168425-64-7
- 英文名:
- COMPOUND 401
- 英文别名:
- CS-315;Morpholino a;Compound 401, >=98%;COMPOUND401;COMPOUND-401;2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one;2-(Morpholin-4-yl)pyrimido[2,1-a]isoquinolin-4-one;2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one>2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one;4H-PyriMido[2,1-a]isoquinolin-4-one, 2-(4-Morpholinyl)-;2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one
- 中文名:
- COMPOUND 401
- 中文别名:
- 化合物COMPOUND 401;2-吗啉-4H-嘧啶并[2,1-A]异喹啉-4-酮;2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮;2-(吗啉-4-基)嘧啶并[2,1-A]异喹啉-4-酮;2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮;2-MORPHOLINO-4H-PYRIMIDO[2,1-A]ISOQUINOLIN-4-ONE 2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮
- CBNumber:
- CB02458229
- 分子式:
- C16H15N3O2
- 分子量:
- 281.31
- MOL File:
- 168425-64-7.mol
|
|
|
COMPOUND 401化学性质
-
熔点:
-
184-186℃ (ethanol )
-
|
-
沸点:
-
456.9±55.0 °C(Predicted)
-
|
-
密度:
-
1.36±0.1 g/cm3 (20 ºC 760 Torr)
-
|
-
储存条件:
-
Store at RT
-
|
-
溶解度:
-
DMSO : 6 mg/mL (21.33 mM; Need ultrasonic and warming)
-
|
-
酸度系数(pKa):
-
1.01±0.20(Predicted)
-
|
-
形态:
-
powder to crystal
-
|
-
颜色:
-
White to Light yellow
-
|
-
CAS 数据库:
-
168425-64-7
-
|
COMPOUND 401性质、用途与生产工艺
Compound 401是DNA-PK和mTOR抑制剂(IC50分别为0.28 μM和5.3 μM)。它对p110α/p85α PI3K没有明显抑制作用,在COS7细胞中抑制S6激酶在Thr389位的磷酸化和Akt在Ser473位的磷酸化。
Target | Value |
DNA-PK
(Cell-free assay)
|
0.28 μM
|
mTOR
(Cell-free assay)
|
5.3 μM
|
Compound 401 is a potent inhibitor of DNA-PK (IC
50
=0.28 μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC
50
=5.3 μM) but not p110α/p85α PI3K (IC
50
>100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr
389
and Akt Ser
473
, respectively). By contrast, there is no direct inhibition of Akt Thr
308
phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5 μM or 10 μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1
-/-
fibroblasts is inhibited in the presence of Compound 401, but TSC1
+/+
cells are resistant.
COMPOUND 401
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 | M2537 | 2-吗啉基-4H-嘧啶并[2,1-a]异喹啉-4-酮 2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one | 168425-64-7 | 10mg | 250元 |
2024/04/30 | M2537 | 2-吗啉基-4H-嘧啶并[2,1-a]异喹啉-4-酮 2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one | 168425-64-7 | 50mg | 955元 |
168425-64-7, COMPOUND 401 相关搜索:
- 高端化学
- 抑制剂
- 重氮化合物
- 偶氮
- 叠氮
- 2-吗啉-4H-嘧啶并[2,1-A]异喹啉-4-酮
- 化合物COMPOUND 401
- 2-MORPHOLINO-4H-PYRIMIDO[2,1-A]ISOQUINOLIN-4-ONE 2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮
- 2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮
- 2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮
- 2-(吗啉-4-基)嘧啶并[2,1-A]异喹啉-4-酮
- 168425-64-7
- DNA-PK,Compound401,DNA-dependent protein kinase,Compound-401,Compound 401,inhibit,Inhibitor
- Morpholino a
- 2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one>
- COMPOUND401;COMPOUND-401
- CS-315
- 2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one
- Compound 401, >=98%
- 2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one
- 2-(Morpholin-4-yl)pyrimido[2,1-a]isoquinolin-4-one
- 4H-PyriMido[2,1-a]isoquinolin-4-one, 2-(4-Morpholinyl)-
- 2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one