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ATM&ATR

AZD0156 (1821428-35-6)

AZD0156 is an oral, potent and selective ATM kinase inhibitor, inhibiting the kinase activity of ATM and ATM-mediated signaling, preventing DNA damage checkpoint activation, and disrupting DNA damage repair, inducing tumor cell apoptosis, and leading to cell death in ATM-overexpressing tumor cells…

Not Intended for Therapeutic Use. For research use only.

CAS: 1821428-35-6 Category

AZD0156 (1821428-35-6) Description:

AZD0156 is an orally bioavailable ataxia telangiectasia mutated (ATM) kinase inhibitor, with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, AZD0156 targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, AZD0156 sensitizes tumor cells to chemo- and radiotherapy.

AZD0156 (1821428-35-6) Specifications:

Product Name AZD0156
Synonym AZD0156; AZD-0156; AZD 0156.
Chemical Name 8-[6-[3-(dimethylamino)propoxy]-3-pyridyl]-3-methyl-1-tetrahydropyran-4-yl-imidazo[4,5-c]quinolin-2-one
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1821428-35-6
Molecular Formula C26H31N5O3
Molecular Weight 461.566
Monoisotopic Mass 461.2427 g/mol
MDL number MFCD30470661
InChIKey AOTRIQLYUAFVSC-UHFFFAOYSA-N
InChi Code InChI=1S/C26H31N5O3/c1-29(2)11-4-12-34-24-8-6-19(16-28-24)18-5-7-22-21(15-18)25-23(17-27-22)30(3)26(32)31(25)20-9-13-33-14-10-20/h5-8,15-17,20H,4,9-14H2,1-3H3
SMILES O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=C(OCCCN(C)C)N=C5)=CC=C4N=C3
Form Powder
Color White to off-white
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application Torin-1 is a potent and selective mTOR inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Targeting the kinase activities of ATR and ATM exhibits antitumoral activity in mouse models of MLL-rearranged AML. Morgado-Palacin I, Day A, Murga M, Lafarga V, Anton ME, Tubbs A, Chen HT, Ergan A, Anderson R, Bhandoola A, Pike KG, Barlaam B, Cadogan E, Wang X, Pierce AJ, Hubbard C, Armstrong SA, Nussenzweig A, Fernandez-Capetillo O. Sci Signal. 2016 Sep 13;9(445):ra91. doi: 10.1126/scisignal.aad8243. PMID: 27625305.

[2]. pRAD50: a novel and clinically applicable pharmacodynamic biomarker of both ATM and ATR inhibition identified using mass spectrometry and immunohistochemistry. Jones GN, Rooney C, Griffin N, Roudier M, Young LA, Garcia-Trinidad A, Hughes GD, Whiteaker JR, Wilson Z, Odedra R, Zhao L, Ivey RG, Howat WJ, Harrington EA, Barrett JC, Ramos-Montoya A, Lau A, Paulovich AG, Cadogan EB, Pierce AJ. Br J Cancer. 2018 Nov;119(10):1233-1243. doi: 10.1038/s41416-018-0286-4. Epub 2018 Nov 2. PMID: 30385821.

[3].Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors. Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, Goldberg K, Hassall LA, Hughes GD, MacFaul PA, McGuire TM, Pass M, Patel A, Pearson S, Petersen J, Pike KG, Robb G, Stratton N, Xin G, Zhai B. ACS Med Chem Lett. 2018 Jul 13;9(8):809-814. doi: 10.1021/acsmedchemlett.8b00200. eCollection 2018 Aug 9. PMID: 30128072.