(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide
KU-60019
CAS: 925701-49-1
Molecular Formula: C30H33N3O5S
(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide - Names and Identifiers
(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide - Physico-chemical Properties
| Molecular Formula | C30H33N3O5S |
| Molar Mass | 547.66512 |
| Density | 1.314 |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | -20°C |
| In vitro study | KU-55933 is an improved water-soluble inhibitor of ATM kinase with an IC50 of 6.3 nM and a similar target-specific selectivity compared to an IC50 of 13 nM at KU-60019 ATM. KU-60019 had little activity at DNA-PKcs and ATR, with IC50 of 1.7 μm and> 10 μm, and no activity at 229 other protein kinases, such as PI3K, mTOR/fkbp12. Blocking radiation-induced phosphorylation of key ATM protein targets such as p53,γ-H2AX, and CHK2 in human glioma U87 and U1242 cells, KU-60019 was 3 to 10 times more potent than KU-55933, 1 M KU-60019 significantly induced p53(S15) phosphorylation decreased by more than 70%, and ~ 10 M KU-55933 to achieve the same degree of reduction. KU-60019 to effectively make human glioma cells radiosensitization, 1 μm and 10 μm treatment, dose enhancement ratio were 1.7 and 4.4, normal fibroblasts, but not A- T fibroblasts, were also radiosensitized. 3 μm KU-60019 inhibited basal and insulin-induced phosphorylation of AKT S473 by 70% and-50%, respectively, and completely reduced radiation-induced phosphorylation of AKT to below control levels. The effect of KU-60019 on AKT S473 phosphorylation was observed in glioma cell lines and normal fibroblasts but not in A- T(h-TERT) cells, and was effectively inhibited by the phosphatase inhibitor okadaic acid, the key role of ATM kinase in the regulation of AKT phosphorylation is illustrated. Consistent with inhibition of pro-survival AKT signaling, 3 μm KU-60019 significantly inhibited migration and invasion of human glioma U87 cells by> 70% and ~ 60%, respectively, and also inhibited migration and invasion of U1242 cells, inhibition was> 50% and-60%, respectively. |
| In vivo study | In orthotopic glioma U1242/luc-GFP xenograft models, the combination of KU-60019 and radiation significantly increases survival of mice than KU-60019 alone, radiation alone, or no treatment. In addition, p53-mutant gliomas is much more sensitive to KU-60019 radiosensitization than wild-type glioma. |
(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.826 ml | 9.129 ml | 18.259 ml |
| 5 mM | 0.365 ml | 1.826 ml | 3.652 ml |
| 10 mM | 0.183 ml | 0.913 ml | 1.826 ml |
| 5 mM | 0.037 ml | 0.183 ml | 0.365 ml |
Last Update：2024-01-02 23:10:35
(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide - Introduction
KU-60019 is a chemical substance whose chemical name is 2,6-bis(hydroxymethyl)-9-(2-morpholin-4-ethyl) -1,8-dimethyl-9h-purine-2, 4-dione.
Nature:
KU-60019 is a colorless crystalline solid, soluble in organic solvents (such as methanol, ethanol, etc.) and some polar solvents. Its chemical structure contains multiple hydroxyl functional groups.
Use:
KU-60019 is a DNA-dependent protein kinase (pi3k-related protein kinase) inhibitor. It can be used in biomedical research, mainly for the Study of apoptosis, DNA damage repair and cell cycle regulation and other fields.
Preparation Method:
The preparation method of KU-60019 is more complicated, and organic synthesis methods are generally used. Specific methods vary by manufacturer and researcher.
Safety Information:
The safety data of the KU-60019 is limited, so strict safety operation measures are required during use. In general, direct contact should be avoided and work should be done in a well-ventilated laboratory environment. At the same time, the waste should be treated and disposed according to the actual experimental conditions and safe operation specifications. Before use, it is recommended to read the relevant safety data sheet and technical instructions, and follow the instructions. In case of discomfort or accident, seek medical attention immediately.
Nature:
KU-60019 is a colorless crystalline solid, soluble in organic solvents (such as methanol, ethanol, etc.) and some polar solvents. Its chemical structure contains multiple hydroxyl functional groups.
Use:
KU-60019 is a DNA-dependent protein kinase (pi3k-related protein kinase) inhibitor. It can be used in biomedical research, mainly for the Study of apoptosis, DNA damage repair and cell cycle regulation and other fields.
Preparation Method:
The preparation method of KU-60019 is more complicated, and organic synthesis methods are generally used. Specific methods vary by manufacturer and researcher.
Safety Information:
The safety data of the KU-60019 is limited, so strict safety operation measures are required during use. In general, direct contact should be avoided and work should be done in a well-ventilated laboratory environment. At the same time, the waste should be treated and disposed according to the actual experimental conditions and safe operation specifications. Before use, it is recommended to read the relevant safety data sheet and technical instructions, and follow the instructions. In case of discomfort or accident, seek medical attention immediately.
Last Update：2024-04-09 21:11:58
![(2R,6S)-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide](http://res.chembk.com/assets/images/structure/311863.gif)
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Product Name: KU-60019 Visit Supplier Webpage Request for quotation
CAS: 925701-49-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 925701-49-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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