Lanabecestat(AZD3293)

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.
Targets
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].

Protocol

Cell Research:

[1]

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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:

[1]

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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
Formula

C26H28N4O

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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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BACE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID