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ATM&ATR

AZ20 (1233339-22-4)

AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR. AZ20 is an ATR protein kinase inhibitor,….

Not Intended for Therapeutic Use. For research use only.

CAS: 1233339-22-4 Category

AZ20 (1233339-22-4) Description:

AZ20 is an ATR protein kinase inhibitor, which inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC50 of 5 nM and ATR mediated phosphorylation of Chk1 in HT29 colorectal adenocarcinoma tumor cells with an IC50 of 50 nM. AZ20 potently inhibits the growth of LoVo colorectal adenocarcinoma tumor cells in vitro and has high free exposure in mouse following moderate oral doses. AZ20 is a useful compound to explore ATR pharmacology in vivo.

AZ20 (1233339-22-4) Specifications:

Product Name AZ20
Synonym AZ20; AZ-20; AZ 20.
Chemical Name (R)-4-(2-(1H-indol-4-yl)-6-(1-(methylsulfonyl)cyclopropyl)pyrimidin-4-yl)-3-methylmorpholine
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1233339-22-4
Molecular Formula C21H24N4O3S
Molecular Weight 412.51
Monoisotopic Mass 412.15691 g/mol
MDL number MFCD25976730
InChIKey SCGCBAAYLFTIJU-CQSZACIVSA-N
InChi Code InChI=1S/C21H24N4O3S/c1-14-13-28-11-10-25(14)19-12-18(21(7-8-21)29(2,26)27)23-20(24-19)16-4-3-5-17-15(16)6-9-22-17/h3-6,9,12,14,22H,7-8,10-11,13H2,1-2H3/t14-/m1/s1
SMILES C[[email protected]]1N(C2=NC(C3=CC=CC4=C3C=CN4)=NC(C5(S(=O)(C)=O)CC5)=C2)CCOC1
Form Powder
Color 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 AZ20 is an ATR protein kinase inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Mechanisms responsible for the synergistic antileukemic interactions between ATR inhibition and cytarabine in acute myeloid leukemia cells. Ma J, Li X, Su Y, Zhao J, Luedtke DA, Epshteyn V, Edwards H, Wang G, Wang Z, Chu R, Taub JW, Lin H, Wang Y, Ge Y. Sci Rep. 2017 Feb 8;7:41950. doi: 10.1038/srep41950. PMID: 28176818.

[2]. Inhibition of ATR potentiates the cytotoxic effect of gemcitabine on pancreatic cancer cells through enhancement of DNA damage and abrogation of ribonucleotide reductase induction by gemcitabine. Liu S, Ge Y, Wang T, Edwards H, Ren Q, Jiang Y, Quan C, Wang G. Oncol Rep. 2017 Jun;37(6):3377-3386. doi: 10.3892/or.2017.5580. Epub 2017 Apr 19. PMID: 28440428.

[3].Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent. Foote KM, Nissink JWM, McGuire T, Turner P, Guichard S, Yates JWT, Lau A, Blades K, Heathcote D, Odedra R, Wilkinson G, Wilson Z, Wood CM, Jewsbury PJ. J Med Chem. 2018 Nov 21;61(22):9889-9907. doi: 10.1021/acs.jmedchem.8b01187. Epub 2018 Nov 10. PMID: 30346772.

[4]. Susceptibility of Pseudaletia unipuncta (Lepidoptera: Noctuidae) to entomopathogenic nematodes (Rhabditida: Steinernematidae and Heterorhabditidae) isolated in the Azores: effect of nematode strain and host age. Medeiros J, Rosa JS, Tavares J, Simões N. J Econ Entomol. 2000 Oct;93(5):1403-8. PMID: 11057710.