WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407113
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.
MedKoo Cat#: 407113
Chemical Formula: C19H18N4O2
Exact Mass: 334.14298
Molecular Weight: 334.38
Elemental Analysis: C, 68.25; H, 5.43; N, 16.76; O, 9.57
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
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|
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.