产品说明书

NU 7026

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Chemical Structure| 154447-35-5 同义名 : LY293646;DNA-PK Inhibitor II
CAS号 : 154447-35-5
货号 : A183964
分子式 : C17H15NO3
纯度 : 98+%
分子量 : 281.306
MDL号 : MFCD06798345
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 2 mg/mL(7.11 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

1% DMSO+30% polyethylene glycol+1% Tween 80+water 30 mg/mL suspension

生物活性
靶点
  • PI3K

    PI3K, IC50:13 μM

  • DNA-PK

    DNA-PK, IC50:0.23 μM

描述 NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM[1]. NU7026 enhances the cytotoxic effects of ionizing radiation (IR) in cells proficient in DNA-PK, evidenced by a potentiation factor at 90% cell kill (PF90) of 1.51±0.04[1]. In vitro, at a 10 μM concentration, which itself is not toxic to cells, NU7026 4-hour exposure combined with 3 Gy of radiation to significantly increase radiosensitivity in CH1 human ovarian cancer cells[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HeLa cells Function assay Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50=0.23 μM 15658870
HeLa cells Function assay Inhibition of mTOR protein isolated from HeLa cells, IC50=6.4 μM 15658870
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.55mL

7.11mL

3.55mL

参考文献

[1]Veuger SJ, et al. Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1. Cancer Res. 2003 Sep 15;63(18):6008-15.

[2]Nutley BP, et al. Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026. Br J Cancer. 2005 Oct 31;93(9):1011-8.