AZD1080|cas 612487-72-6|DC Chemicals

Cas No.:	612487-72-6
Chemical Name:	Azd1080
Synonyms:	AZD1080;2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-1H-indole-5-carbonitrile;3-[5-(morpholin-4-ylmethyl)-1H-pyridin-2-ylidene]-2-oxo-1H-indole-5-carbonitrile;AZD 1080;AZD-1080;0TII45R8IJ;AZD 1080;AK198951;2-hydroxy-3-(5-(morpholinomethyl)pyridin-2-yl)-1H-indole-5-carbonitrile;2-Hydroxy-3-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]-1H-indole-5-carbonitrile;1H-INDOLE-5-CARBONITRILE, 2-HYDROXY-3-[5-(4-MORPHOLINYLMETHYL)-2-PYRIDINYL]-;2-Hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1H-indole-5-carbonitrile;(3Z)-3-[5-(Morpholin-4-ylmethyl)-1H-pyridin-2-ylidene]-2-oxo-1H-indole-5-carbonitrile;1H-Indole-5-carbonitril
SMILES:	O1C([H])([H])C([H])([H])N(C([H])([H])C2=C([H])N=C(C([H])=C2[H])C2=C(N([H])C3C([H])=C([H])C(C#N)=C([H])C2=3)O[H])C([H])([H])C1([H])[H]
Formula:	C₁₉H₁₈N₄O₂
M.Wt:	334.3718
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
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[1].
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 (pKi< 5; >10 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[1].

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