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ApexBio/AZD0156/5mg/B7822

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¥9760.00
货号:B7822
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品牌:ApexBio
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AZD0156ATM kinase inhibitor

Catalog No.B7822
SizePriceStockQty
5mg
$68.00
In stock
25mg
$208.00
In stock
100mg
$488.00
In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Publications citing ApexBio Products

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)594-8
Nat Nanotechnol.2017 Dec;12(12):1190-1198.
Nature Biotechnology.2017 Jun;35(6):569-576
Nat 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):312-323
Nat 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

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

AZD0156 Dilution Calculator

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AZD0156 Molarity Calculator

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Chemical Properties

Cas No. 1821428-35-6SDF 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 AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request
General tipsFor 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.

Background

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

ApexBio的3X FLAG Peptide FLAG标签系统利用与目标蛋白质1融合的短而亲水的8个氨基酸的肽段。FLAG肽与抗体M1结合。结合是钙依赖性方式2还是非依赖性3仍存在争议。该系统的缺点是单克隆抗体纯化基质不如其他基质稳定。通常,可以用特异性单克隆抗体检测小标签。为了改善对FLAG标签的检测,已经开发了3x FLAG系统。这种三级FLAG表位是亲水的,长22个氨基酸,可以检测到高达10 fmol的表达融合蛋白。激烈热球菌的带有FLAG标签的麦芽糖糊精结合蛋白已被结晶4,其晶体质量与未标记蛋白的晶体质量非常相似。 最后,可以通过用肠激酶处理去除FLAG标签,肠激酶对肽序列5的5个C末端氨基酸具有特异性。