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LRRK2-kinase inhibitor

Product Name
LRRK2-kinase inhibitor
CAS No.
1285515-21-0
Chemical Name
LRRK2-kinase inhibitor
Synonyms
CS-1790;GSK2578215;SK2578215A;GSK257821A;GSK2578125A;GSK2578215A;GSK2578215A, >=98%;GSK2578215A ，S7664;LRRK2-kinase inhibitor;GSK2578215A >=98% (HPLC)
CBNumber
CB92628049
Molecular Formula
C24H18FN3O2
Formula Weight
399.42
MOL File
1285515-21-0.mol
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LRRK2-kinase inhibitor Property

Boiling point:
556.1±50.0 °C(Predicted)
Density 
1.292±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: soluble15mg/mL, clear
form 
powder
pka
12.31±0.70(Predicted)
color 
white to beige
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0660
Product name
GSK2578215A
Purity
≥98% (HPLC)
Packaging
5mg
Price
$122
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0660
Product name
GSK2578215A
Purity
≥98% (HPLC)
Packaging
25mg
Price
$496
Updated
2025/07/31
Cayman Chemical
Product number
14603
Product name
GSK2578215A
Purity
≥98%
Packaging
5mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
14603
Product name
GSK2578215A
Purity
≥98%
Packaging
10mg
Price
$107
Updated
2024/03/01
Cayman Chemical
Product number
14603
Product name
GSK2578215A
Purity
≥98%
Packaging
25mg
Price
$249
Updated
2024/03/01
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LRRK2-kinase inhibitor Chemical Properties,Usage,Production

Uses

GSK2578215A is a potent, selective LRRK2 inhibitor and a promising therapeutic for treating Parkinson''s disease.

Biological Activity

GSK2578215A is a potent inhibitor of leucine-rich repe at kinase-2 (LRRK2) also known as dardarin or PARK8, a kinase with mutations linked to Parkinson′s disease. Because the most common mutation, G2019S, enhances LRRK2 kinase activity, it is hoped th at LRRK2 inhibitors may be useful in treating the disease. GSK2578215A inhibited both wild-type and G2019S mutant LRRK2 kinase activity with IC50s of 10.9 and 8.9 nM respectively. It has good blood-brain barrier (BBB) permeability with a high ratio of brain to plasma distribution in mice.', 'GSK2578215A stimulates mitochondrial fragmentation, autophagy and mitophagy.

Synthesis

1285513-32-7

401815-98-3

1285515-21-0

Compound (CAS: 1285513-32-7) (771 mg, 2.012 mmol) and 2-fluoro-4-pyridineboronic acid (425 mg, 3.02 mmol) were used as raw materials in the presence of bis(triphenylphosphine)palladium(II) chloride (70.6 mg, 0.101 mmol) and sodium carbonate (1066 mg, 10.06 mmol), and in a solvent mixture of DME (20 mL) and water (2 mL) was stirred at reflux for 2 hours. After completion of the reaction, the mixture was diluted with ethyl acetate (50 mL) and water (50 mL). The organic layer was separated and the aqueous layer was extracted with ethyl acetate (50 mL x 2). The organic layers were combined, concentrated, and the crude product was purified by silica gel column chromatography using 0-10% methanol/dichloromethane (containing 1% ammonia) as eluent to afford 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide (500 mg, 1.252 mmol, 62.2% yield) as an off-white solid.

in vivo

GSK2578215A (5 mg/kg, i.p.) with Olaparib (HY-10162) (50?mg/kg, i.p., T.I.W for 3 weeks) effectively inhibits the tumor growth in mice bearing OVCAR8 xenografts[3].
GSK2578215A (IV, 1 mg/kg, or PO, 10 mg/kg) achieves an exposure in the brain with a brain to plasma ratio of 1.4 (IV) and 2.4 (PO), and shows low oral bioavailability (IV, 12.2%), a half-life of 1.14 h (IV) and plasma exposure (PO, 635.3 h ng/mL, AUClast)[1].

Animal Model:mice bearing OVCAR8 xenografts[3]
Dosage:5 mg/kg, with Olaparib (50?mg/kg)
Administration:i.p., for 3 weeks
Result:Inhibited the tumor growth and increased DNA damage in tumors more potently than Olaparib or GSK2578215A alone.

storage

Store at RT

References

[1] Bioorganic and Medicinal Chemistry Letters, 2017, vol. 27, # 17, p. 4034 - 4038
[2] Patent: WO2011/38572, 2011, A1. Location in patent: Page/Page column 158; 159

LRRK2-kinase inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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LRRK2-kinase inhibitor Suppliers

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View Lastest Price from LRRK2-kinase inhibitor manufacturers

Career Henan Chemical Co
Product
LRRK2-kinase inhibitor 1285515-21-0
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
20kg
Release date
2019-12-23

1285515-21-0, LRRK2-kinase inhibitorRelated Search:


  • LRRK2-kinase inhibitor
  • CS-1790
  • LRRK2 inhibitor GS2578215A
  • GSK2578215A, >=98%
  • 2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzaMide
  • 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide GSK2578215A
  • 5-(2-fluoro-4-pyridinyl)-2-[(phenylmethyl)oxy]-N-3-pyridinylbenzamide
  • GSK2578125A
  • BenzaMide, 5-(2-fluoro-4-pyridinyl)-2-(phenylMethoxy)-N-3-pyridinyl-
  • GSK2578215A
  • 5-(2-Fluoro-4-pyridinyl)-2-(phenylmethoxy)-N-3-pyridinylbenzamide
  • 5-(2-Fluoropyridin-4-yl)-2-phenylmethoxy-N-pyridin-3-ylbenzamide
  • GSK2578215
  • SK2578215A
  • GSK2578215A >=98% (HPLC)
  • LRRK2 inhibitor GSK2578215A
  • LRRK2-kinase inhibitor USP/EP/BP
  • GSK2578215A, LRRK2 inhibitor
  • GSK2578215A, 10 mM in DMSO
  • GSK257821A
  • GSK2578215A (GSK-2578215A)
  • GSK2578215A ，S7664
  • 5-(2-Fluoropyridin-4-yl)-2-(benzyloxy)-N-pyridin-3-ylbenzamide
  • 1285515-21-0
  • C24H18FN3O2
  • Inhibitors