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Details

Stereochemistry ACHIRAL
Molecular Formula C19H18N4O2
Molecular Weight 334.3718
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AZD-1080

SMILES

OC1=C(C2=C(N1)C=CC(=C2)C#N)C3=NC=C(CN4CCOCC4)C=C3

InChI

InChIKey=BLTVBQXJFVRPFK-UHFFFAOYSA-N
InChI=1S/C19H18N4O2/c20-10-13-1-3-16-15(9-13)18(19(24)22-16)17-4-2-14(11-21-17)12-23-5-7-25-8-6-23/h1-4,9,11,22,24H,5-8,12H2

HIDE SMILES / InChI

Molecular Formula C19H18N4O2
Molecular Weight 334.3718
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

AZ-1080 (AZD-1080) is an inhibitor of GSK-beta which was developed by AstraZeneca and initially tested in patients with Alzheimer’s disease (phase I). The drug was discontinued for the aforementioned condition, but now it is being investigated as a potential therapy for ovarina cancer and emdometrial carcinoma (basic research).

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
31.0 nM [Ki]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
86 nM
15 mg 1 times / day steady-state, oral
AZD-1080 plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
20 h
15 mg 1 times / day steady-state, oral
AZD-1080 plasma
Homo sapiens

Doses

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​

PubMed

Sample Use Guides

In Vivo Use Guide
Middle-aged subjects (45–64 years) receive 15 mg AZ-1080 once daily for 14 days.
Route of Administration: Oral
In Vitro Use Guide
3T3 fibroblasts stably expressing human tau protein were treated with 1 uM of AZ-1080. Dose-dependent inhibition of tau phosphorylation was observed for AZ-1080 with IC50 value of 324 nM.
Substance Class Chemical
Record UNII
0TII45R8IJ
Record Status Validated (UNII)
Record Version