Name: Lanabecestat (AZD3293)
Brand: Selleck Chemicals
SKU: S8193
Availability: InStock
Rating: 5 (6 reviews)

Jump to

Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE)
Other BACE Inhibitors	Verubecestat (MK-8931) LY2811376 LY2886721 Verubecestat (MK-8931) Trifluoroacetate AZD3839 Elenbecestat LX2343 Loganin Dieckol

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (198.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.100mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.025mg/ml (2.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 20.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	412.53	Formula	C₂₆H₂₈N₄O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1383982-64-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY3314814			SMILES	CC#CC1=CC(=CN=C1)C2=CC3=C(CC4(C35N=C(C(=N5)N)C)CCC(CC4)OC)C=C2

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	BACE (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 this compound with respect to secretion of Aβ40 and sAβPPβ is studied in a range of cellular models, it 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). It 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. 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 t_1/2 of approximately 9 h.
In vivo	Lanabecestat (AZD3293) displays significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ in vivo in mice, guinea pigs, and dogs. In the dog PK study, its bioavailability is determined to be 80% (F = 0.8). The preclinical data strongly support the clinical development of this compound, and patients with AD are currently being recruited into a combined Phase 2/3 study to test its disease-modifying properties.
References	[1] https://pubmed.ncbi.nlm.nih.gov/26890753/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2018-06-28)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03545087	WITHDRAWN	Renal Insufficiency	Eli Lilly and Company	2018-06	PHASE1
NCT02245737	TERMINATED	Alzheimer´s Disease	AstraZeneca	2014-09-30	PHASE2; PHASE3
NCT02972658	TERMINATED	Alzheimer's Disease	AstraZeneca	2017-03-15	PHASE3
NCT03506399	WITHDRAWN	Healthy	Eli Lilly and Company	2018-06	PHASE1
NCT02783573	TERMINATED	Alzheimer's Disease	AstraZeneca	2016-07-01	PHASE3
NCT03499041	Withdrawn	Hepatic Impairment	Eli Lilly and Company\|AstraZeneca	2018-06	Phase 1

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Lanabecestat (AZD3293) BACE inhibitor

Chemical Structure

Molecular Weight: 412.53