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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
KU-60019 is an improved analogue of KU-55933 with 10-fold higher activity than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. It is a very potent radiosensitizer with an IC50 of 6.3 nM for ATM in cell-free assays, and it is 270 and 1600 times more selective for ATM than DNA-PK and ATR. In human glioma cell lines that are p53 wild type (U87) and p53 mutant (U1242), KU-60019 can decrease radiation-induced S473 AKT phosphorylation. But AKT suppression does not improve KU-60019's radiosensitization. In human glioma cells U87 and U1242, KU-60019 has been shown to inhibit cell migration and invasion in a dose-dependent manner. Furthermore, it has been demonstrated that KU-60019 can inhibit the growth of U1242 cells to a certain degree.
Targets |
ATM ( IC50 = 6.3 nM ); DNA-PKcs ( IC50 = 1.7 μM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
KU-60019 is exposed to cells for 1, 3, and 5 days. AlamarBlue is the measure of cell growth. The medium is supplemented with AlamarBlue up to the suggested final concentration. The Fluoro-Count plate reader (excitation 530 nm, emission 590 nm) is used to measure fluorescence on the plates after an hour of incubation at 37 °C. The values obtained represent the growth of the cells. The trypan blue/fluorescence activated cell sorting (FACS) assay is used to assess cell survival.
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Animal Protocol |
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References |
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Molecular Formula |
C30H33N3O5S
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Molecular Weight |
547.67
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Exact Mass |
547.21
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CAS # |
925701-49-1
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Related CAS # |
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Appearance |
Powder
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SMILES |
C[C@@H]1CN(C[C@@H](O1)C)CC(=O)NC2=CC3=C(C=C2)SC4=C(C3)C=CC=C4C5=CC(=O)C=C(O5)N6CCOCC6
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InChi Key |
SCELLOWTHJGVIC-BGYRXZFFSA-N
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InChi Code |
InChI=1S/C30H33N3O5S/c1-19-16-32(17-20(2)37-19)18-28(35)31-23-6-7-27-22(13-23)12-21-4-3-5-25(30(21)39-27)26-14-24(34)15-29(38-26)33-8-10-36-11-9-33/h3-7,13-15,19-20H,8-12,16-18H2,1-2H3,(H,31,35)/t19-,20+
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Chemical Name |
2-[(2S,6R)-2,6-dimethylmorpholin-4-yl]-N-[5-(6-morpholin-4-yl-4-oxopyran-2-yl)-9H-thioxanthen-2-yl]acetamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
5%DMSO+ 40%PEG300+5%Tween 80+50%ddH2O: 5.0mg/ml (9.13mM) (Please use freshly prepared in vivo formulations for optimal results.)
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Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
KU-60019 is a more effective inhibitor of the ATM kinase than KU-55933.Mol Cancer Ther.2009 Oct;8(10):2894-902. th> |
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KU-60019 radiosensitizes U87 and U1242 human glioma cells and normal but not A-T fibroblasts.Mol Cancer Ther.2009 Oct;8(10):2894-902. td> |
KU-60019 inhibits migration and invasion of human glioma U87 and U1242 cells in vitro.Mol Cancer Ther.2009 Oct;8(10):2894-902. td> |