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KU60019

KU60019

产品编号 T2474   CAS 925701-49-1
别名: KU-60019, KU 60019

KU60019 是一种有效的、可逆的 ATM 激酶抑制剂 (IC50: 6.3 nM)。它对一组 229 种其他激酶的效果要差得多或没有效果。

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KU60019 Chemical Structure
KU60019, CAS 925701-49-1
规格 价格/CNY 货期 数量
1 mg ¥ 297 现货
5 mg ¥ 710 现货
10 mg ¥ 990 现货
25 mg ¥ 1,980 现货
50 mg ¥ 2,930 现货
1 mL * 10 mM (in DMSO) ¥ 920 现货
其他形式的 KU60019:
产品目录号及名称: KU60019 (T2474)
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选择批次  
纯度: 99.14% ee: 100%
纯度: 98.79% ee: 100%
纯度: 98%
纯度: 95.9%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases.
靶点活性 ATM:6.3 nM (cell free)
体外活性 KU-60019 is an improved inhibitor of the ATM kinase with an IC50 of 6.3 nM, approximately half that of KU-55933. The IC50 values for DNA-PKcs and ATR are 1.7 and >10 μM, respectively, almost 270-and 1600-fold higher than for ATM [1]. KU-60019 at 300 nM completely inhibited p53 and H2AX phosphorylation as quickly as 15 min after application. When U1242 cells were treated with KU-60019 for 1 h, washed to remove KU-60019 and then challenged with IR, the inhibitory effects of KU-60019 were reversed as early as 15 min after washout [2].
体内活性 Despite PTEN-deficient control tumors reaching a 4-fold increase in size before PTEN wild-type controls, KU-60019–treated PTEN-deficient tumors displayed a statistically significant slowing in growth. This growth inhibition was especially evident at the start of the experiment (days 5–12) just after KU-60019 was administered (days 1–5) [3]. When mice harboring U1242/luc-GFP tumors were treated with KU-60019 administered from an osmotic pump followed by 2 Gy of irradiation, we were able to demonstrate a complete elimination of tumor cells on day 20 by bioluminescence imaging (BLI) 7 days after radiation [4].
细胞实验 Cell growth was determined by AlamarBlue. U1242 cells were serially diluted, allowed to attach for 6 h and then exposed to KU-60019 at 3 μM. At days 1, 3 and 5 after seeding, AlamarBlue was added to the medium to the recommended final concentration. Plates were incubated for 1 h at 37°C and fluorescence determined on a FluoroCount plate reader (excitation 530 nm, emission 590 nm) and values taken as a measure of cell growth [1].
动物实验 Cells (3 × 10^7) were implanted into male Fox Chase Severe Combined Immunodeficiency (SCID) mice. Administration of doxycycline was started when tumors reached 100 mm3 in volume and was performed every 48 hours up to removal of the animal from the experiment. Forty-eight hours after PTEN induction, animals were administered KU-60019 (100 mg/kg) for 5 consecutive days and measured until they reached a target 400 mm3 volume. Measurements of tumor volume and body weight took place every 3 days using calipers [3].
别名 KU-60019, KU 60019
分子量 547.67
分子式 C30H33N3O5S
CAS No. 925701-49-1

存储

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

溶解度

DMSO: 15 mg/mL (27.4 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

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 1.8259 mL 9.1296 mL 18.2592 mL 45.6479 mL
5 mM 0.3652 mL 1.8259 mL 3.6518 mL 9.1296 mL
10 mM 0.1826 mL 0.913 mL 1.8259 mL 4.5648 mL
20 mM 0.0913 mL 0.4565 mL 0.913 mL 2.2824 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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Golding SE, et al. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion. Mol Cancer Ther. 2009 Oct;8(10):2894-902. 2. Golding SE, et al. Dynamic inhibition of ATM kinase provides a strategy for glioblastoma multiforme radiosensitization and growth control. Cell Cycle. 2012 Mar 15;11(6):1167-73. 3. McCabe N, et al. Mechanistic Rationale to Target PTEN-Deficient Tumor Cells with Inhibitors of the DNA Damage Response Kinase ATM. Cancer Res. 2015 Jun 1;75(11):2159-65. 4. Biddlestone-Thorpe L, et al. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15;19(12):3189-200. 5. Liang J, Niu Z, Yu X, et al. Counteracting Genome Instability by p53-dependent Mintosis[J]. bioRxiv. 2020. 6. Liang J, Niu Z, Zhang B, et al. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis[J]. Cell Death & Differentiation. 2020: 1-15. 7. Ha G H, Ji J H, Chae S, et al. Pellino1 regulates reversible ATM activation via NBS1 ubiquitination at DNA double-strand breaks[J]. Nature communications. 2019 Apr 5;10(1):1577.

文献引用

1. Ha G H, Ji J H, Chae S, et al. Pellino1 regulates reversible ATM activation via NBS1 ubiquitination at DNA double-strand breaks. Nature communications. 2019 Apr 5;10(1):1577. 2. Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15 3. Liang J, Niu Z, Zhang B, et al Liang J, Niu Z, Zhang B, et al. p53-dependent elimination of aneuploid mitotic offspring by entosis. Cell Death & Differentiation. 2020: 1-15. 4. Qiao S, Lu W, Glorieux C, et al. Wild-type IDH2 protects nuclear DNA from oxidative damage and is a potential therapeutic target in colorectal cancer. Oncogene. 2021: 1-13.
CGK733 AZD0156 Ro 90-7501 (Z)-Mirin GJ103 sodium salt Dactolisib Elimusertib Schisandrin B

相关化合物库

该产品包含在如下化合物库中:
PI3K/Akt/mTOR 化合物库 神经再生化合物库 细胞重编程化合物库 NO PAINS 化合物库 HIF-1化合物库 表型筛选靶点鉴定库 氧化还原化合物库 癌细胞分化化合物库 糖代谢化合物库 酪氨酸激酶分子库

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
g
给药体积
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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。
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计算 重置

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

KU60019 925701-49-1 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling ATM/ATR KU-60019 KU 60019 Inhibitor inhibitor inhibit

 

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