NU 7026 (LY293646) 是一种新型特异性的 D

NU 7026  (Synonyms: LY293646)

NU 7026 (LY293646) 是一种新型特异性的 DNA-PK 抑制剂，IC₅₀ 为 0.23 μM，也抑制 PI3K，IC₅₀ 为 13 μM。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

生物活性    
NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.

体外研究
(In Vitro)    
NU7026 (10 μM) potentiates ionizing radiation (IR) cytotoxicity [potentiation factor at 90% cell kill (PF90)=1.51±0.04] in exponentially growing DNA-PK proficient but not deficient cells[1]. NU7026 synergistically sensitizes I83 cells to Chlorambucil (CLB) 3.5-fold[2].NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). At a dose of 10 μM, which is nontoxic to cells per se, a minimum NU7026 exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells[3].
Solution in vitro: NU7026 is dissolved in anhydrous DMSO. NU7026 is added to cells to a final concentration of 0.25% DMSO (v/v)[4].

体内研究
(In Vivo)    
NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). Following intravenous administration to mice at 5 mg/kg, NU7026 underwent rapid plasma clearance (0.108 L/h) and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration at 20 mg/kg is 20 and 15%, respectively[3].
Solution in vivo:
NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline (i.p. and p.o.) (Mice)[3].
NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline (i.v.)[3].

分子量    
281.31

性状    
Solid

Formula    
C17H15NO3

CAS 号    
154447-35-5

运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
Powder    -20°C    3 years
4°C    2 years
In solvent    -80°C    6 months
-20°C    1 month
溶解性数据    
In Vitro: 
DMSO : 2.5 mg/mL (8.89 mM; Need ultrasonic)

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    3.5548 mL    17.7740 mL    35.5480 mL
5 mM    0.7110 mL    3.5548 mL    7.1096 mL
10 mM    ---    ---    ---
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
 

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.  [Content Brief] [2]. Amrein L, et al. Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase. J  [Content Brief] [3]. 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.  [Content Brief] [4]. Ciszewski WM, et al. Interleukin-4 enhances PARP-dependent DNA repair activity in vitro. J Interferon Cytokine Res. 2014 Sep;34(9):734-40. [Content Brief]