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AZD1080

CAT: 0013-GTR19161245-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161245-01Size:200 mg
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Description
AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. (In Vitro) :AZD1080 shows selectivity against cdk2 (pKi=5.9; 1150 nM; 37-fold), cdk5 (pKi=6.4; 429 nM; 14-fold), cdk1 (pKi=5.7; 1980 nM; 64-fold) and Erk2 (pKi10 μM; >323-fold) . AZD1080 (at 10 μM) is also evaluated for pan-kinase selectivity and showed good overall selectivity versus 23 kinases, as well as against 65 different receptors, enzymes and ion channels in MDS Pharma screen (< 50% effect at 10 μM AZD1080) . Concentration-dependent inhibition of tau phosphorylation is observed for AZD1080 (IC50=324 nM) and the non-selective reference GSK3 inhibitor LiCl (IC50=1.5 mM) indicating that AZD1080 is several orders of magnitude more potent than LiCl. (In Vivo) :The pharmacokinetic analysis in blood after oral administration revealed that AZD1080 has a good oral bioavailability in rats (15-24%) with a half-life of 7.1 h, making AZD1080 attractive for further in vivo testing. The subchronic (3 days) oral treatment with AZD1080 at 4 or 15 μmol/kg significantly blocked the MK-801-induced memory deficit (AZD1080 vs. MK-801, p<0.05 at 4 μmol/kg and p<0.01 at 15 μmol/kg) in mice, raising the hypothesis that longer treatment may be required to prime the synapses to function effectively.
CAS Number
612487-72-6
Product Name Alternative
AZD-1080 | AZD 1080 | AZD-1080
Purity
>98% (HPLC)
Solubility
DMSO: 52 mg/mL (155.51 mM)
Smiles
N#CC1=CC2=C (NC (/C2=C3C=CC (CN4CCOCC4) =CN/3) =O) C=C1
Molecular Formula
C19H18N4O2
Molecular Weight
334.37
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
(Z) -3- (5- (morpholinomethyl) pyridin-2 (1H) -ylidene) -2-oxoindoline-5-carbonitrile

Chemical Information

Azd-1080

AZD1080 is a member of the class of hydroxyindoles that is 1H-indole substituted by hydroxy, 5-(morpholin-4-ylmethyl)pyridin-2-yl, and cyano groups at positions 2, 3 and 5, respectively. It is a potent, brain permeable inhibitor of human GSK3alpha and GSK3beta with Ki of 6.9 nM and 31 nM, respectively. The drug was being developed by AstraZeneca for the treatment of Alzheimer's disease (clinical trial now discontinued). It has a role as a tau aggregation inhibitor, an antineoplastic agent, an apoptosis inducer and an EC 2.7.11.26 (tau-protein kinase) inhibitor. It is a nitrile, a member of pyridines, a member of morpholines, a tertiary amino compound and a member of hydroxyindoles.

CAS Number612487-72-6
PubChem CID135564570
IUPAC Name2-hydroxy-3-[5-(morpholin-4-ylmethyl)-2-pyridinyl]-1H-indole-5-carbonitrile
Molecular FormulaC19H18N4O2
Molecular Weight334.4
XLogP1.8
Topological Polar Surface Area85.2
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count3
Heavy Atom Count25
Formal Charge0
Complexity501
SMILES
C1COCCN1CC2=CN=C(C=C2)C3=C(NC4=C3C=C(C=C4)C#N)O
InChI
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
InChIKey
BLTVBQXJFVRPFK-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Azd-1080
CAS: 612487-72-6
CID: 135564570
Formula: C19H18N4O2
MW: 334.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight334.4
XLogP31.8
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count3
Exact Mass334.14297583
Monoisotopic Mass334.14297583
Topological Polar Surface Area85.2 Ų
Heavy Atom Count25
Formal Charge0
Complexity501
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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TRC-A808085-100MGAZD1080
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A12819-100AZD1080 100mg

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