| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
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.
| 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].
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| 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].
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| 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 |
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| Molecular Formula |
C24H18FN3O2
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|---|---|---|
| Molecular Weight |
399.42
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| Exact Mass |
399.138
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| CAS # |
1285515-21-0
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| Related CAS # |
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| PubChem CID |
68107965
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
556.1±50.0 °C at 760 mmHg
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| Flash Point |
290.1±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.651
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
543
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WCIGMFCFPXZRMQ-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
5-(2-fluoropyridin-4-yl)-2-phenylmethoxy-N-pyridin-3-ylbenzamide
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| Synonyms |
GSK-2578215A; GSK 2578215A; GSK2578215A; 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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.
(2) Be sure to add the solvent(s) in order.
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