|2-((2R,6S)-rel-2,6-二甲基吗啉基)-N-(5-(6-吗啉基-4-氧代-4H-吡喃-2-基)-9H-噻吨-2-基)乙酰胺|CsnPharm

CAS No.: 925701-46-8

KU-60019 Catalog No. CSN15844

Synonyms: Ku-60019

KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The serine/threonine protein kinase ATM signals can regulate cell cycle and DNA repair components through phosphorylation on the targets such as p53, CHK2, NBS1, and BRCA1, thus playing a central role in the maintenance of genome integrity. KU-60019 is an improved inhibitor of the ATM kinase (compared with KU-55933) with an IC50 of 6.3 nM. Pre-treatment with KU-60019 can inhibit the downstream targets p53 phosphorylation at Ser15 site, as well as CHK2 at T68 site, induced by 5Gy of ionizing radiation in U1242 cells. Compared with KU-55933, KU-60019 acts as a more potent radiosensitizer at concentration>1 μM in U87 and U1242 human glioma cells but not A-T fibroblasts. Treatment with KU-60019 resulted in inhibited migration of U87 cells ≥70% in a dose-dependent manner and inhibited invasion of U1242 cells by ∼60%, which may due to the impaired AKT signaling^[1]. In in vivo study, combination of radiation and KU-60019 administrated by pump implantation at dose of 10μM, significantly increase survival of mice 2- to 3-fold over controls in orthotopic human glioma xenograft models^[2].
作用机制KU-60019 is an improved form of KU-55933, which is an ATP-competitive ATM inhibitor.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
BAECs	10 μM	Function Assay	1 h	abolishes the phosphorylation of ATM-Ser1981	25498542
BAECs	10 μM	Function Assay	1 h	inhibits the increase in NOS activity	25498542
U1242	3 μM	Kinase Assay	0.5 h	inhibits the ATM kinase	23620409

更多
动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.), 100 mg/kg^[4]

给药途径
i.p.
临床研究

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.), 100 mg/kg^[4]
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03571438	Kidney Cancer	Not Applicable	Recruiting	September 30, 2024	France ... more >> Grenoble Alps Hospital Recruiting Grenoble, France, 38043 Contact: Jean-Luc Descotes, PU-PH Collapse <<

参考文献

[1] Golding SE, Rosenberg E, 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] Biddlestone-Thorpe L, Sajjad M, et al. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15;19(12):3189-200.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8259 mL
- 9.1296 mL
- 18.2592 mL
- 5 mM
- 0.3652 mL
- 1.8259 mL
- 3.6518 mL
- 10 mM
- 0.1826 mL
- 0.9130 mL
- 1.8259 mL

技术信息

CAS号

925701-46-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H33N3O5S

运输

蓝冰

分子量

547.67

别名

Ku-60019

溶解度

DMSO	200.0 mg/mL (365.2 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	4 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

KU-60019 Catalog No. CSN15844

靶点选择性

请登录您的专属账户

确认信息