KU 60019 manufacturers
- KU-60019
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2026-07-14
- CAS:925701-46-8
- Purity: 98.05%
- Supply Ability: 10g
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| | KU 60019 Basic information |
| Product Name: | KU 60019 | | Synonyms: | (2R,6S)-rel-2,6-Dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-4-morpholineacetamide;2-((2R,6S)-2,6-Dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl;KU-60019
(KU60019;4-Morpholineacetamide, 2,6-dimethyl-N-[5-[6-(4-morpholinyl)-4-oxo-4H-pyran-2-yl]-9H-thioxanthen-2-yl]-, (2R,6S)-rel-;2-((2R,6S)-2,6-Dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl)acetamide;ATM Inhibitor, KU 60019 | | CAS: | 925701-46-8 | | MF: | C30H33N3O5S | | MW: | 547.67 | | EINECS: | | | Product Categories: | | | Mol File: | 925701-46-8.mol |  |
| | KU 60019 Chemical Properties |
| 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 | | InChIKey | SCELLOWTHJGVIC-BGYRXZFFSA-N | | SMILES | S1c2c(cccc2C5=CC(=O)C=C(O5)N6CCOCC6)Cc3c1ccc(c3)NC(=O)CN4C[C@H](O[C@H](C4)C)C |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | KU 60019 Usage And Synthesis |
| 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 |
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