COMPOUND 401
- CAS号:168425-64-7
- 英文名:COMPOUND 401
- 中文名:COMPOUND 401
- CBNumber:CB02458229
- 分子式:C16H15N3O2
- 分子量:281.31
- MOL File:168425-64-7.mol
- 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
- 海关编码 :2934.99.4400
COMPOUND 401性质、用途与生产工艺
- 生物活性 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。
-
靶点
Target Value DNA-PK
(Cell-free assay)0.28 μM mTOR
(Cell-free assay)5.3 μM -
体外研究
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.
- 更新日期:2024/04/30
- 产品编号:M2537
- 产品名称: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
- CAS编号:168425-64-7
- 包装:10mg
- 价格:250元
- 更新日期:2024/04/30
- 产品编号:M2537
- 产品名称: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
- CAS编号:168425-64-7
- 包装:50mg
- 价格:955元
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