WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406441
CAS#: 925701-46-8
Description: KU-60019 is a potent and selective ATM inhibitor. KU-60019 is 10-fold more effective than KU-55933 at blocking radiation-induced phosphorylation of key ATM targets in human glioma cells. As expected, KU-60019 is a highly effective radiosensitizer of human glioma cells. KU-60019 inhibits the DNA damage response, reduces AKT phosphorylation and prosurvival signaling, inhibits migration and invasion, and effectively radiosensitizes human glioma cells
Hodoodo Cat#: H406441
Name: KU-60019
CAS#: 925701-46-8
Chemical Formula: C30H33N3O5S
Exact Mass: 547.21
Molecular Weight: 547.670
Elemental Analysis: C, 65.79; H, 6.07; N, 7.67; O, 14.61; S, 5.85
Synonym: KU60019; KU 60019; KU-60019.
IUPAC/Chemical Name: 2-((2S,6R)-2,6-dimethylmorpholino)-N-(5-(6-morpholino-4-oxo-4H-pyran-2-yl)-9H-thioxanthen-2-yl)acetamide.
InChi Key: SCELLOWTHJGVIC-BGYRXZFFSA-N
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+
SMILES Code: O=C(NC1=CC(CC2=C(C(C3=CC(C=C(N4CCOCC4)O3)=O)=CC=C2)S5)=C5C=C1)CN6C[C@H](C)O[C@H](C)C6
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 547.67 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Vecchio D, Daga A, Carra E, Marubbi D, Baio G, Neumaier CE, Vagge S, Corvò R, Pia Brisigotti M, Louis Ravetti J, Zunino A, Poggi A, Mascelli S, Raso A, Frosina G. Predictability, efficacy and safety of radiosensitization of glioblastoma-initiating cells by the ATM inhibitor KU-60019. Int J Cancer. 2013 Dec 19. doi: 10.1002/ijc.28680. [Epub ahead of print] PubMed PMID: 24443327.
2: Zirkin S, Davidovich A, Don J. The PIM-2 kinase is an essential component of the ultraviolet damage response that acts upstream to E2F-1 and ATM. J Biol Chem. 2013 Jul 26;288(30):21770-83. doi: 10.1074/jbc.M113.458851. Epub 2013 Jun 11. PubMed PMID: 23760264; PubMed Central PMCID: PMC3724634.
3: Biddlestone-Thorpe L, Sajjad M, Rosenberg E, Beckta JM, Valerie NC, Tokarz M, Adams BR, Wagner AF, Khalil A, Gilfor D, Golding SE, Deb S, Temesi DG, Lau A, O'Connor MJ, Choe KS, Parada LF, Lim SK, Mukhopadhyay ND, Valerie K. ATM kinase inhibition preferentially sensitizes p53-mutant glioma to ionizing radiation. Clin Cancer Res. 2013 Jun 15;19(12):3189-200. doi: 10.1158/1078-0432.CCR-12-3408. Epub 2013 Apr 25. PubMed PMID: 23620409; PubMed Central PMCID: PMC3687028.
4: Golding SE, Rosenberg E, Adams BR, Wignarajah S, Beckta JM, O'Connor MJ, Valerie K. Dynamic inhibition of ATM kinase provides a strategy for glioblastoma multiforme radiosensitization and growth control. Cell Cycle. 2012 Mar 15;11(6):1167-73. doi: 10.4161/cc.11.6.19576. Epub 2012 Mar 15. PubMed PMID: 22370485; PubMed Central PMCID: PMC3335919.
5: Gamper AM, Choi S, Matsumoto Y, Banerjee D, Tomkinson AE, Bakkenist CJ. ATM protein physically and functionally interacts with proliferating cell nuclear antigen to regulate DNA synthesis. J Biol Chem. 2012 Apr 6;287(15):12445-54. doi: 10.1074/jbc.M112.352310. Epub 2012 Feb 23. PubMed PMID: 22362778; PubMed Central PMCID: PMC3320994.
6: Raso A, Vecchio D, Cappelli E, Ropolo M, Poggi A, Nozza P, Biassoni R, Mascelli S, Capra V, Kalfas F, Severi P, Frosina G. Characterization of glioma stem cells through multiple stem cell markers and their specific sensitization to double-strand break-inducing agents by pharmacological inhibition of ataxia telangiectasia mutated protein. Brain Pathol. 2012 Sep;22(5):677-88. doi: 10.1111/j.1750-3639.2012.00566.x. Epub 2012 Feb 21. PubMed PMID: 22257080.
7: Golding SE, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA, O'Connor MJ, Povirk LF, van Meter T, Valerie K. 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. doi: 10.1158/1535-7163.MCT-09-0519. Epub 2009 Oct 6. PubMed PMID: 19808981; PubMed Central PMCID: PMC2761990.
