| AZD0156ATM kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.94%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
AZD0156 Dilution Calculator
calculate
AZD0156 Molarity Calculator
calculate
| Cas No. | 1821428-35-6 | SDF | Download SDF |
| Chemical Name | 8-(6-(3-(dimethylamino)propoxy)pyridin-3-yl)-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinolin-2(3H)-one | ||
| Canonical SMILES | O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3 | ||
| Formula | C26H31N5O3 | M.Wt | 461.56 |
| Solubility | ≥23.1mg/mL in DMSO with gentle warming, ≥5.49mg/mL in EtOH | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AZD0156 is an ATM kinase inhibitor.
Ataxia telangiectasia mutant (ATM), a serine/threonine protein kinase from the phosphatidylinositol 3-kinase-related kinase (PIKK) family of protein kinases, plays a critical role in the cellular DNA damage response signalling activated by DNA double strand breaks. Activated ATM can promote DNA repair and S/G1-cell cycle checkpoints to prevent premature mitosis, maintain genomic integrity as well as promote appropriate cell survival or death pathways. Thus, ATM inhibitor can represent a promosing clinical opportunity to hyper-sensitize tumors to chemo/radiotherapy.
In vitro: AZD0156 was identified as a first in class orally available ATM inhibitor, showing sub-nanomolar potency in cell based assays of ATM inhibition. Moreover, AZD0156 had selectivities of greater than 1000 fold over other members of the PIKK family enzymes [1].
In vivo: In animal study, AZD0156 displayed excellent preclinical PK properties including oral bioavailability. Additionally, in mouse xenograft models, AZD0156 showed robust efficacy after oral administration when combined with double strand breaks (DSB) inducing agents [1].
Clinical trial: AZD0156 is now undergoing early clinical assessment to investigate the safety and preliminary efficacy at increasing doses alone or in combination with other anti-cancer treatment in patients with advanced cancer [2].
References:[1] Kurt G. Pike. Identifying high quality, potent and selective inhibitors of ATM kinase: Discovery of AZD0156. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 4859.[2] https://clinicaltrials.gov/ct2/show/NCT02588105 term=AZD0156&rank=1
