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GSK-2269557

Product Name
GSK-2269557
CAS No.
1254036-77-5
Chemical Name
GSK-2269557
Synonyms
CS-2463;GSK-2269557;GSK2269557 HCL;GSK-2269557 HCl salt;GSK-2269557 (Nemiralisib HCl);2-(6-(1H-Indol-4-yl)-1H-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazole hydrochloride;6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride;6-(1H-Indol-4-yl)-4-[5-[[4-(1-methylethyl)-1-piperazinyl]methyl]-2-oxazolyl]-1H-indazole hydrochloride (1:1);1H-Indazole, 6-(1H-indol-4-yl)-4-[5-[[4-(1-methylethyl)-1-piperazinyl]methyl]-2-oxazolyl]-, hydrochloride (1:1)
CBNumber
CB52704697
Molecular Formula
C26H29ClN6O
Formula Weight
477.00106
MOL File
1254036-77-5.mol
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GSK-2269557 Property

storage temp. 
Store at -20°C
solubility 
≤0.2mg/ml in ethanol;20mg/ml in DMSO;14mg/ml in dimethyl formamide
form 
crystalline solid
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17388
Product name
GSK2269557
Purity
≥98%
Packaging
1mg
Price
$40
Updated
2024/03/01
Cayman Chemical
Product number
17388
Product name
GSK2269557
Purity
≥98%
Packaging
5mg
Price
$177
Updated
2024/03/01
Cayman Chemical
Product number
17388
Product name
GSK2269557
Purity
≥98%
Packaging
10mg
Price
$312
Updated
2024/03/01
Cayman Chemical
Product number
17388
Product name
GSK2269557
Purity
≥98%
Packaging
25mg
Price
$680
Updated
2024/03/01
ApexBio Technology
Product number
C5012
Product name
GSK2269557
Packaging
25mg
Price
$776
Updated
2021/12/16
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GSK-2269557 Chemical Properties,Usage,Production

Biological Activity

pki : 9.9gsk2269557 is an inhibitor of pi3kδ.phosphoinositide 3-kinase delta (pi3kδ), a lipid kinase belonging to the class 1 pi3k family, catalyzes the phosphorylation of phosphatidylinositol-4,5-bisphosphate to produce the critical signalling molecule phosphatidylinositol-3,4,5-triphosphate and then triggers various downstream biological events that ultimately regulate cell proliferation, growth, differentiation, chemotaxis and survival.

in vitro

in the screening study, gsk2269557 met the original potency goal in the pbmc assay (pic50 >9) and showed exquisite selectivity against the pi3k isoforms in a modified htrf assay. moreover, gsk2269557 could induce concentration-dependent increases in qt interval and tpe at 0.3 and 1 μm and an increase in qrs at 1 μm, however, no treatment-related tdp arrhythmias were seen [1].

in vivo

in a disease relevant brown norway rat acute ova model of th2 driven lung inflammation, gsk2269557 was found to be albe to protect against eosinophil recruitment with an ed50 of 67 μg/kg. the activity of gsk2269557 was also assessed using other endpoints, leukocyte recruitment to the lung (neutrophils, macrophages, cd4 and cd8 t-lymphocytes at 48 hours) and th2 cytokines such as il-13. it was found that gsk2269557 could reduce recruitment of all leukocyte subpopulations and il-13 in the lungs in a dose-dependent manner [1].

References

[1] down, k. ,amour, a.,baldwin, i.r., et al. optimization of novel indazoles as highly potent and selective inhibitors of phosphoinositide 3-kinase δ for the treatment of respiratory disease. j. med. chem. 58(18), 7381-7399 (2015).
[2] robert wilson, anthony cahn, amanda deans, iain mcsherry, curtis rambaran, ana sousa, darren wilbraham. safety, tolerability and pharmacokinetics (pk) of single and repeat nebulised doses of a novel phosphoinositide 3-kinase δ inhibitor (pi3kδ), gsk2269557, administered to healthy male subjects in a phase i study. european respiratory journal 2013 42: p729.

GSK-2269557 Preparation Products And Raw materials

Raw materials

Preparation Products

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GSK-2269557 Suppliers

Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9926
Advantage
65
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View Lastest Price from GSK-2269557 manufacturers

Career Henan Chemical Co
Product
6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride 1254036-77-5
Price
US $1.00/KG
Min. Order
1KG
Purity
Min98% HPLC
Supply Ability
g/kg/ton
Release date
2019-12-20

1254036-77-5, GSK-2269557Related Search:


  • GSK-2269557
  • 2-(6-(1H-Indol-4-yl)-1H-indazol-4-yl)-5-((4-isopropylpiperazin-1-yl)methyl)oxazole hydrochloride
  • GSK2269557 HCL
  • 6-(1H-Indol-4-yl)-4-[5-[[4-(1-methylethyl)-1-piperazinyl]methyl]-2-oxazolyl]-1H-indazole hydrochloride (1:1)
  • GSK-2269557 HCl salt
  • 6-(1H-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1H-indazole hydrochloride
  • CS-2463
  • GSK-2269557 (Nemiralisib HCl)
  • 1H-Indazole, 6-(1H-indol-4-yl)-4-[5-[[4-(1-methylethyl)-1-piperazinyl]methyl]-2-oxazolyl]-, hydrochloride (1:1)
  • 1254036-77-5
  • C26H28N6OHCl
  • C26H29ClN6O