GSK2578215A

Alias: GSK-2578215A; GSK 2578215A; GSK2578215A; 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide
Cat No.:V0775 Purity: ≥98%
GSK2578215A (GSK-2578215A; GSK 2578215A;GSK-2578215 A) is a novel, highly potent and selective LRRK2 kinase inhibitor with anti-PD (Parkinsons disease) activity.
GSK2578215A Chemical Structure CAS No.: 1285515-21-0
Product category: LRRK2
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GSK2578215A (GSK-2578215A; GSK 2578215A; GSK-2578215 A) is a novel, highly potent and selective LRRK2 kinase inhibitor with anti-PD (Parkinson's disease) activity. It inhibits LRRK2 (G2019S) and LRRK2 (WT) with an IC50 of 8.9 nM and 10.9 nM, respectively.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
GSK2578215A (0-1 μM, 90 minutes) inhibits the phosphorylation of Ser910 and Ser935 in mouse Swiss 3T3 cells [1] and HEK293 cells that have been stably transfected with wild-type LRRK2 and LRRK2[G2019S]. In SH-SY5Y cells, GSK2578215A (1 nM, 12 hours) induces autophagy (increased levels of LC3 and p62 protein) [2]. In SH-SY5Y cells, GSK2578215A (1 nM, 12 hours) causes Drp1-mediated mitochondrial fission as well as mitophagy (12 and 24 hours) [2]. In SH-SY5Y cells, GSK2578215A (1 nM, 24 hours) causes oxidative stress, which is reflected in the accumulation of 4-HNE, and causes apoptosis [2]. In OVCAR8 cells, GSK2578215A (1 μM, 24 hours) inhibits homologous recombination [3].
ln Vivo
In mice with OVCAR8 xenografts, GSK2578215A (5 mg/kg, i.p.) and olaparib (50 mg/kg, i.p., TIW for 3 weeks) can both efficiently reduce tumor growth [3]. With a brain exposure (brain/plasma exposure ratio) of 1.4 (IV) and 2.4 (PO) and a low oral bioavailability (IV, 12.2%), half-life of 1.14 hours (IV), and plasma exposure (PO, 635.3 h·ng/mL, AUClast), GSK2578215A (IV, 1 mg/kg or PO, 10 mg/kg) exhibits these characteristics [1].
Animal Protocol
Animal/Disease Models: mice bearing OVCAR8 xenografts[3]
Doses: 5 mg/kg, with Olaparib (50 mg/kg)
Route of Administration: ip, for 3 weeks
Experimental Results: Inhibited the tumor growth and increased DNA damage in tumors more potently than Olaparib or GSK2578215A alone.
References
[1]. Reith AD, et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5625-9.
[2]. Saez-Atienzar S, et al. The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 2014 Aug 14;5(8):e1368.
[3]. Chen L, et al. LRRK2 inhibition potentiates PARP inhibitor cytotoxicity through inhibiting homologous recombination-mediated DNA double strand break repair. Clin Transl Med. 2021 Mar;11(3):e341.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H18FN3O2
Molecular Weight
399.42
CAS #
1285515-21-0
SMILES
O=C(NC1=CC=CN=C1)C2=CC(C3=CC(F)=NC=C3)=CC=C2OCC4=CC=CC=C4
InChi Key
WCIGMFCFPXZRMQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H18FN3O2/c25-23-14-19(10-12-27-23)18-8-9-22(30-16-17-5-2-1-3-6-17)21(13-18)24(29)28-20-7-4-11-26-15-20/h1-15H,16H2,(H,28,29)
Synonyms
GSK-2578215A; GSK 2578215A; GSK2578215A; 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 79 mg/mL (197.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5036 mL 12.5182 mL 25.0363 mL
5 mM 0.5007 mL 2.5036 mL 5.0073 mL
10 mM 0.2504 mL 1.2518 mL 2.5036 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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