KU 60019
- Product Name
- KU 60019
- CAS No.
- 925701-46-8
- Chemical Name
- KU 60019
- Synonyms
- KU-60019 (KU60019;ATM Inhibitor, KU 60019;2-((2R,6S)-2,6-Dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl;2-((2R,6S)-2,6-Dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl)acetamide;(2R,6S)-rel-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide;4-Morpholineacetamide, 2,6-dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-, (2R,6S)-rel-
- CBNumber
- CB72535679
- Molecular Formula
- C30H33N3O5S
- Formula Weight
- 547.67
- MOL File
- 925701-46-8.mol
KU 60019 Property
- Boiling point:
- 786.6±60.0 °C(Predicted)
- Density
- 1.314±0.06 g/cm3 (20 ºC 760 Torr)
- storage temp.
- Store at -20°C
- solubility
- DMF:20.0(Max Conc. mg/mL);36.52(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);0.91(Max Conc. mM)
DMSO:75.0(Max Conc. mg/mL);136.94(Max Conc. mM)
Ethanol:50.0(Max Conc. mg/mL);91.3(Max Conc. mM) - form
- A crystalline solid
- pka
- 13.52±0.20(Predicted)
- color
- Light yellow to khaki
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 17502
- Product name
- Ku-60019
- Packaging
- 1mg
- Price
- $29
- Updated
- 2024/03/01
- Product number
- 17502
- Product name
- Ku-60019
- Packaging
- 25mg
- Price
- $250
- Updated
- 2024/03/01
- Product number
- 17502
- Product name
- Ku-60019
- Packaging
- 5mg
- Price
- $115
- Updated
- 2024/03/01
- Product number
- 17502
- Product name
- Ku-60019
- Packaging
- 10mg
- Price
- $143
- Updated
- 2024/03/01
- Product number
- K660435
- Product name
- KU-60019
- Packaging
- 10mg
- Price
- $235
- Updated
- 2021/12/16
KU 60019 Chemical Properties,Usage,Production
Description
Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins. It is much less effective or without effect against a panel of 229 other kinases. Ku-60019 sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro. It produces radiosensitization and increases survival in vivo when administered intra-tumorally in orthotopic xenograft models of glioblastoma multiforme. Ku-60019 is particularly effective in producing lethality in cells with mutant p53 or that are deficient in PTEN.
Uses
KU-60019 is a potent and reversible inhibitor of ATM kinase, blocking the phosphorylation of ATM substrate proteins. It sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro.
in vivo
Despite PTEN-deficient control tumors reaching a 4-fold increase in size before PTEN wild-type controls, KU-60019-treated PTEN-deficient tumors display a statistically significant slowing in growth. This growth inhibition is especially evident at the start of the experiment (days 5-12) just after KU-60019 is administered (days 1-5)[2].
IC 50
ATM: 6.3 nM (IC50); DNA-PKcs: 1.7 μM (IC50)
References
[1] SARAH E GOLDING. Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion.[J]. Molecular Cancer Therapeutics, 2009: 2894-2902. DOI: 10.1158/1535-7163.mct-09-0519
[2] SARAH E GOLDING. Dynamic inhibition of ATM kinase provides a strategy for glioblastoma multiforme radiosensitization and growth control.[J]. Cell Cycle, 2012, 11 6: 1167-1173. DOI: 10.4161/cc.11.6.19576
[3] LAURA BIDDLESTONE-THORPE. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation.[J]. Clinical Cancer Research, 2013, 19 12: 3189-3200. DOI: 10.1158/1078-0432.ccr-12-3408
[4] NUALA MCCABE. Mechanistic Rationale to Target PTEN-Deficient Tumor Cells with Inhibitors of the DNA Damage Response Kinase ATM.[J]. Cancer research, 2015: 2159-2165. DOI: 10.1158/0008-5472.can-14-3502
KU 60019 Preparation Products And Raw materials
Raw materials
Preparation Products
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