For research use only.

Catalog No.S8193 Synonyms: LY3314814

4 publications

Lanabecestat(AZD3293) Chemical Structure

Molecular Weight(MW): 412.53

Lanabecestat (AZD3293, LY3314814) is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor with an inhibitory constant Ki of 0.4 nM.

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Selleck's Lanabecestat(AZD3293) has been cited by 4 publications

1 Customer Review

  • Kinetic studies of known inhibitors against BACE1. a Time courses of BACE1 activity in the presence of different concentrations of AZD3839. b Time courses of BACE1 activity in the presence of different concentrations of AZD3293. c Plot of kobs as a function of inhibitor concentration for the slow binding inhibitor AZD3293. d Reversibility assays with BACE1 and inhibitors using spin column method. The data of reversibility assays were performed in duplicate.

    Anal Bioanal Chem, 2017, 409(28):6635-6642. Lanabecestat(AZD3293) purchased from Selleck.

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Biological Activity

Description Lanabecestat (AZD3293, LY3314814) is an oral beta-secretase 1 cleaving enzyme (BACE) inhibitor with an inhibitory constant Ki of 0.4 nM.
BACE [1]
(Cell-free assay)
0.4 nM(Ki)
In vitro

Lanabecestat(AZD3293, LY3314814)is a potent, highly permeable, orally active, blood-brain barrier (BBB) penetrating, BACE1 inhibitor with unique slow off-rate kinetics. When the potency of AZD3293 with respect to secretion of Aβ40 and sAβPPβ is studied in a range of cellular models, the compound displays pM potency in primary neuron cultures from mice and guinea pigs and in SH-SY5Y cells over-expressing AβPP (IC50 = 610 pM, 310 pM, and 80 pM, respectively). AZD3293 is also tested in a panel of more than 350 in vitro radioligand binding and enzyme activity assays, covering a diverse range of receptors, ion channels, transporters, kinases, and enzymes, up to a concentration of 10μM of AZD3293. A few significant responses are observed, but these had at least a 1,000-fold selectivity against BACE1, thus indicating specificity to BACE1. The off-rate of AZD3293 has an estimated t1/2 of approximately 9 h[1].

In vivo In vivo in mice, guinea pigs, and dogs, AZD3293 displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. In the dog PK study, the bioavailability of AZD3293 is determined to be 80% (F = 0.8). The preclinical data strongly support the clinical development of AZD3293, and patients with AD are currently being recruited into a combined Phase 2/3 study to test the disease-modifying properties of AZD3293[1].


Cell Research:


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  • Cell lines: SH-SY5Y, SH-SY5Y overexpressing wild type AβPP, HEK293 cells overexpressing AβPP with the Swedish mutation (K595N/M596L), N2A cells, and primary cortical neurons isolated from fetal C57BL/6 mice (E16) or Dunkin-Hartley guinea pigs (E25-27)
  • Concentrations: --
  • Incubation Time: 5 to 16 h
  • Method:

    The cells are incubated with different AZD3293 concentrations for 5 to 16 h, and the release of sAβPPβ, Aβ1-40, Aβ1-42, or sAβPPα into the medium is analyzed using specific commercial ELISA or kits from Meso Scale Discovery.

    (Only for Reference)
Animal Research:


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  • Animal Models: C57BL/6 mice
  • Dosages: 50, 100, or 200μmol/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (198.77 mM)
Water Insoluble
Ethanol '82 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 412.53


CAS No. 1383982-64-6
Storage powder
in solvent
Synonyms LY3314814
Smiles CC#CC1=CC(=CN=C1)C2=CC3=C(CC4(C35N=C(C(=N5)N)C)CCC(CC4)OC)C=C2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03499041 Withdrawn Drug: LY3314814 Hepatic Impairment Eli Lilly and Company|AstraZeneca June 2018 Phase 1
NCT03222427 Completed Drug: LY3314814|Drug: [13C415N3] LY3314814 Healthy AstraZeneca|Eli Lilly and Company January 15 2018 Phase 1
NCT03019549 Completed Drug: Lanabecestat|Drug: Rosuvastatin Healthy AstraZeneca|Eli Lilly and Company January 12 2017 Phase 1
NCT02663128 Completed Drug: Lanabecestat Healthy AstraZeneca|Eli Lilly and Company January 31 2016 Phase 1

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BACE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID