AZD-1080 | CAS#612487-72-6 | GSK3 inhibitor |

AZD-1080
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407113

CAS#: 612487-72-6

Description: AZD-1080 is a potent and selective GSK3 inhibitor that demonstrates peripheral target engagement in Phase 1 clinical studies. AZD1080 inhibits tau phosphorylation in cells expressing human tau and in intact rat brain. Interestingly, subchronic but not acute administration with AZD1080 reverses MK-801-induced deficits, measured by long-term potentiation in hippocampal slices and in a cognitive test in mice, suggesting that reversal of synaptic plasticity deficits in dysfunctional systems requires longer term modifications of proteins downstream of GSK3β signaling.

Chemical Structure

AZD-1080

CAS# 612487-72-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407113
Name: AZD-1080
CAS#: 612487-72-6
Chemical Formula: C19H18N4O2
Exact Mass: 334.14
Molecular Weight: 334.380
Elemental Analysis: C, 68.25; H, 5.43; N, 16.76; O, 9.57

Price and Availability

Size	Price	Availability
10mg	USD 150	Ready to ship
25mg	USD 250	Ready to ship
50mg	USD 450	Ready to ship
100mg	USD 750	Ready to ship
200mg	USD 1250	Ready to ship
500mg	USD 1950	Ready to ship
1g	USD 2950	Ready to ship
2g	USD 4850	2 Weeks
5g	USD 7850	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: AZD-1080; AZD 1080; AZD-1080.

IUPAC/Chemical Name: (Z)-3-(5-(morpholinomethyl)pyridin-2(1H)-ylidene)-2-oxoindoline-5-carbonitrile

InChi Key: JULOXTBHCHEFBE-ZCXUNETKSA-N

InChi Code: 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/h1-4,9,11,21H,5-8,12H2,(H,22,24)/b18-17-

SMILES Code: N#CC1=CC2=C(NC(/C2=C3C=CC(CN4CCOCC4)=CN/3)=O)C=C1

Appearance: Orange solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#C7R05B22
View CoA: current batch, Lot#T21D05P06

QC Data:

View QC data: current batch, Lot#C7R05BC22
View QC data: current batch, Lot#T21D05P06

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	AZD1080 is a GSK3 inhibitor with IC50s of 6.9 nM and 31 nM for recombinant human GSK3α and GSK3β, respectively.
In vitro activity:	AZD1080 exposure suppressed ovarian cancer cell proliferation, invasion, migration, and lamellipodia formation, and induced G1 arrest, which was concentration dependent. AZD1080 also significantly downregulated GSK-3β, CDK2, CDK1, cyclin D1, MMP9, and Bcl-xL expression at both mRNA and protein levels. Reference: Drug Des Devel Ther. 2016 Mar 18;10:1225-32. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4807899/
In vivo activity:	The rotarod test, static rod test and pole were used to test the motor function of the PD (Parkinson’s disease) mice. The rotarod test showed MPTP induced a significant loss of latency to fall from the rotarod, and AZD 1080 rescued the time loss induced by MPTP (Figure 8A). MPTP induced an increase in the orientation time and transition time in the static rod test. AZD 1080 shortened the orientation time and transition time compared to the MPTP group (Figure 8B). MPTP increased the time of moving down along the pole. AZD 1080 reversed the increase in the time of moving down induced by MPTP in the pole test (Figure 8C). Reference: Neuropsychiatr Dis Treat. 2020 Mar 4;16:651-663. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7061418/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	25.0	74.77
	DMSO	31.1	93.07
	DMSO:PBS (pH 7.2) (1:1)	0.5	1.50
	Ethanol	0.3	0.75

Preparing Stock Solutions

The following data is based on the product molecular weight 334.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Chen S, Sun KX, Feng MX, Sang XB, Liu BL, Zhao Y. Role of glycogen synthase kinase-3β inhibitor AZD1080 in ovarian cancer. Drug Des Devel Ther. 2016 Mar 18;10:1225-32. doi: 10.2147/DDDT.S102506. PMID: 27051274; PMCID: PMC4807899. 2. Hu S, Hu M, Liu J, Zhang B, Zhang Z, Zhou FH, Wang L, Dong J. Phosphorylation of Tau and α-Synuclein Induced Neurodegeneration in MPTP Mouse Model of Parkinson's Disease. Neuropsychiatr Dis Treat. 2020 Mar 4;16:651-663. doi: 10.2147/NDT.S235562. PMID: 32184604; PMCID: PMC7061418.
In vitro protocol:	1. Chen S, Sun KX, Feng MX, Sang XB, Liu BL, Zhao Y. Role of glycogen synthase kinase-3β inhibitor AZD1080 in ovarian cancer. Drug Des Devel Ther. 2016 Mar 18;10:1225-32. doi: 10.2147/DDDT.S102506. PMID: 27051274; PMCID: PMC4807899.
In vivo protocol:	1. Hu S, Hu M, Liu J, Zhang B, Zhang Z, Zhou FH, Wang L, Dong J. Phosphorylation of Tau and α-Synuclein Induced Neurodegeneration in MPTP Mouse Model of Parkinson's Disease. Neuropsychiatr Dis Treat. 2020 Mar 4;16:651-663. doi: 10.2147/NDT.S235562. PMID: 32184604; PMCID: PMC7061418.

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1: Chen S, Sun KX, Feng MX, Sang XB, Liu BL, Zhao Y. Role of glycogen synthase kinase-3β inhibitor AZD1080 in ovarian cancer. Drug Des Devel Ther. 2016 Mar 18;10:1225-32. doi: 10.2147/DDDT.S102506. eCollection 2016. PubMed PMID: 27051274; PubMed Central PMCID: PMC4807899.

2: Georgievska B, Sandin J, Doherty J, Mörtberg A, Neelissen J, Andersson A, Gruber S, Nilsson Y, Schött P, Arvidsson PI, Hellberg S, Osswald G, Berg S, Fälting J, Bhat RV. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J Neurochem. 2013 May;125(3):446-56. doi: 10.1111/jnc.12203. Epub 2013 Mar 11. PubMed PMID: 23410232.

3: Chen S, Sun KX, Liu BL, Zong ZH, Zhao Y. The role of glycogen synthase kinase-3β (GSK-3β) in endometrial carcinoma: A carcinogenesis, progression, prognosis, and target therapy marker. Oncotarget. 2016 May 10;7(19):27538-51. doi: 10.18632/oncotarget.8485. PubMed PMID: 27050373; PubMed Central PMCID: PMC5053670.

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