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KU-57788

产品编号 T6276 CAS 503468-95-9

别名: NU7441

KU-57788 (NU7441) 是一种 NHEJ 通路抑制剂，抑制 PI3K 和 mTOR，IC50分别为 5.0 和 1.7 μM。它是高效的选择性DNA-PK 抑制剂，IC50为 14 nM。

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KU-57788, CAS 503468-95-9

规格	价格/CNY	货期
2 mg	￥ 263	现货
5 mg	￥ 412	现货
10 mg	￥ 628	现货
25 mg	￥ 1,180	现货
50 mg	￥ 1,980	现货
100 mg	￥ 3,280	现货
500 mg	￥ 7,250	现货
1 mL * 10 mM (in DMSO)	￥ 453	现货

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纯度: 100%

纯度: 99.87%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
靶点活性	DNA-PK:13 nM (cell free)
体外活性	0.3 μM of KU-57788 (NU7441), nontoxic to both normal and tumor cells, caused a significant radio-sensitization in tumor cells exposed to X-rays and carbon ions. This concentration did not seem to cause inhibition of DNA DSB repair but induced a significant G2/M arrest [1]. The addition of NU7441 to cells following introduction of the Cas9/sgGFP editing system and the ΔGFP repair template caused a decrease of approximately 40 % in NHEJ events which was accompanied by an approximately two-fold stimulation in HDR. This effect was dose-dependent and reached a maximum at approximately 2.0 μM for NU7441 [2]. NU7441 reduced the CCK-8 counts in the HepG2 culture, further enhanced 60Cox03B3; radiation injury to HepG2 cells, which was manifested by decreasing the DNA-PKcs (S2056) protein expression, increasing x03B3 [3]. Even though RPA p34 is still localized into foci following UV-irradiation and inhibitor treatment, treatment of cells with NU7441 eliminates staining for hyperphosphorylated RPA p34 [4].
体内活性	Tumors in control mice reached four times their starting volume (RTV4) at a median time of 5.6 days. Treatment with etoposide phosphate alone caused a tumor growth delay of 2.7 days, which was extended to 5.4 days by coadministration of NU7441 [5].
细胞实验	Cells were irradiated with 290 MeV/n carbon ions (LET: 50 keV/μm) at the Heavy Ion Medical Accelerator in Chiba. The dose rate for carbon ions was 1 Gy/min. X‐ray irradiation was performed using a TITAN‐320 (200 kV, 20 mA) at a dose rate of 1 Gy/min. NU7441 was dissolved in DMSO and stored at ?20°C in a freezer. Cells were pretreated with NU7441 1 h before irradiation, and the drug was kept throughout the experiment [1].
动物实验	All in vivo experiments were reviewed and approved by the relevant institutional animal welfare committees and done according to national law. We determined the plasma pharmacokinetics after administering NU7441 i.v. at 5 mg/kg in 10% DMSO/10% cyclodextrin in saline or i.p. or orally at 10 mg/kg (dissolved at 1 mg/mL in 40% PEG400/saline) to female BALB/c mice. These were the maximum administrable doses by the route used due to the limit of solubility of NU7441. Mice were killed at intervals up to 360 minutes after NU7441 administration; blood was taken and immediately centrifuged, and the plasma fraction was removed and stored at ?20°C [5].

别名	NU7441
分子量	413.49
分子式	C25H19NO3S
CAS No.	503468-95-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 14.29 mg/mL (34.56 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4184 mL	12.0922 mL	24.1844 mL	60.461 mL
	5 mM	0.4837 mL	2.4184 mL	4.8369 mL	12.0922 mL
	10 mM	0.2418 mL	1.2092 mL	2.4184 mL	6.0461 mL
	20 mM	0.1209 mL	0.6046 mL	1.2092 mL	3.023 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Sunada S, et al. Nontoxic concentration of DNA-PK inhibitor NU7441 radio-sensitizes lung tumor cells with little effect on double strand break repair. Cancer Sci. 2016 Sep;107(9):1250-5. 2. Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93. 3. Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905. 4. Cruet-Hennequart S, et al. UV-induced RPA phosphorylation is increased in the absence of DNA polymerase eta and requires DNA-PK. DNA Repair (Amst). 2006 Apr 8;5(4):491-504. 5. Zhao Y, et al. Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 2006 May 15;66(10):5354-62. 6. Zhang B, Wu H, Hao J, et al. Inhibition of DNA-PKcs activity re-sensitizes uveal melanoma cells to radio-and chemotherapy[J]. Biochemical and Biophysical Research Communications. 2019

文献引用

1. Zhang B, Wu H, Hao J, et al. Inhibition of DNA-PKcs activity re-sensitizes uveal melanoma cells to radio-and chemotherapy. Biochemical and Biophysical Research Communications. 2019 2. Feng Y L, Liu S C, Chen R D, et al.Proximal binding of dCas9 at a DNA double strand break stimulates homology-directed repair as a local inhibitor of classical non-homologous end joining.Nucleic Acids Research.2023: gkad116.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

KU-57788 503468-95-9 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK CRISPR/Cas9 inhibit DNA-dependent protein kinase NU-7441 Inhibitor NU 7441 NU7441 KU 57788 KU57788 inhibitor

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KU-57788

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords