AZD-0156 Property

Boiling point:

628.3±55.0 °C(Predicted)

Density 

1.242±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥23.1 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥5.49 mg/mL in EtOH

form 

solid

pka

9.27±0.28(Predicted)

color 

White to off-white

Safety

HS Code 

2934999090

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

AZD-0156 Chemical Properties,Usage,Production

Uses

AZD 0156 is an inhibitor of the Ataxia-Telangiectasia Mutated (ATM) protein, a signaling kinase involved in the DNA damage response.

Biological Activity

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].

target

Target	Value
ATM

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