CS-2622

中文名称:

CS-2622

中文同义词:

DNA-PK特异抑制剂(LTURM34);化合物LTURM34

英文名称:

LTURM34

英文同义词:

LTURM34;LTURM 34; LTURM-34;CS-2622;8-(4-Dibenzothienyll)-2-(4-morpholinyl)-4H-1,3-benzoxazin-4-one;4H-1,3-Benzoxazin-4-one, 8-(4-dibenzothienyl)-2-(4-morpholinyl)-

CAS号:

1879887-96-3

分子式:

C24H18N2O3S

分子量:

414.48

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1879887-96-3.mol

储存条件 

Sealed in dry,2-8°C

生物活性

LTURM34 是一种特异的 DNA-PK 抑制剂 (IC50=34 nM)。与 PI3K 相比，LTURM34 对 DNA-PK 的选择性高 170 倍。LTURM34 在多种肿瘤细胞系中显示出有效的抗增殖活性。

靶点

DNA-PK 34 nM (IC 50 ) PI3Kβ 5.8 μM (IC 50 ) PI4Kδ 8.5 μM (IC 50 )

DNA-PK 34 nM (IC 50 )

PI3Kβ 5.8 μM (IC 50 )

体外研究

LTURM34 shows potent inhibition of DNA-PK with excellent selectivity over the Class I PI3K isoforms. The IC 50 s are 5.8 and 8.5 μM for PI3K β and δ, respectively. LTURM34 is more consistently active against the selected cell lines (11 of 16), but at best shows 54% inhibition against the HOP-92 non-small cell lung cancer line.