ChemicalBook > CAS DataBase List > 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione

5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione

Product Name
5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
CAS No.
958852-01-2
Chemical Name
5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
Synonyms
CS-536;CS-1726;GSK-615;CS-1156;SK1059615;GSK 1059615;GSK 1059615;GSK-1059615;PI3K inhibitor GS1059615;GSK1059615, 10 mM in DMSO;GSK 1059615 SodiuM Salt Hydrate
CBNumber
CB62518985
Molecular Formula
C18H11N3O2S
Formula Weight
333.36
MOL File
958852-01-2.mol
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5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione Property

Melting point:
>290°C (dec.)
storage temp. 
Store at +4°C
solubility 
H2O: ≥8mg/mL
form 
powder
color 
yellow
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

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

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

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0083
Product name
GSK 1059615 sodium salt hydrate
Packaging
10 mg
Price
$123
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0083
Product name
GSK 1059615 sodium salt hydrate
Packaging
50 mg
Price
$503
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0083
Product name
GSK 1059615 sodium salt hydrate
Packaging
10mg
Price
$120
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0083
Product name
GSK 1059615 sodium salt hydrate
Packaging
50mg
Price
$489
Updated
2024/03/01
Cayman Chemical
Product number
11569
Product name
GSK1059615
Purity
≥98%
Packaging
5mg
Price
$93
Updated
2024/03/01
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5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione Chemical Properties,Usage,Production

Uses

GSK 1059615 is a potent inhibitor of PI 3-kinase and FRAP (mTOR).

Uses

GSK 1059615 is a potent inhibitor of PI 3-kinase α (PI3Kα). GSK 1059615 inhibits proliferation in BT474 cells and attenuates MAPK signaling.

Definition

ChEBI: GSK1059615 is a thiazolidinone that is the 5-{[4-(pyridin-4-yl)quinolin-6-yl]methylene} derivative of 1,3-thiazolidine-2,4-dione. A PI3K inhibitor It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an antineoplastic agent. It is a member of quinolines, a member of pyridines and a thiazolidinone.

Biological Activity

gsk1059615 is inhibitor of pan-pi3k with ic50 values of 0.4nm, 0.6nm, 5nm, 2nm and 12nm for pi3kα, p13kβ, p13kγ, p13kδ and mtor, respectively [1].gsk1059615 is a potent and reversible inhibitor of p13k. it also has inhibition efficacy to the oncogenic mutants of pi3kα. the thiazolidinedione ring of gsk1059615 forms an interaction with the catalytic lysine (lys833) within the atp-binding pocket. in cellular assay, gsk1059615 is reported to induce g1 arrest and apoptosis in a variety of cell lines. among these, the breast tumor cells display more sensitive. moreover, gsk1059615 significantly suppresses tumor growth and increases plasma insulin levels in xenograft mice [1, 2].

in vivo

GSK1059615 (25 mg/kg) effectively inhibits tumor growth in xenograft mice models of BT474 or HCC1954 breast cancer cells[1].

IC 50

PI3Kα: 0.4 nM (IC50); PI3Kβ: 0.6 nM (IC50); PI3Kγ: 2 nM (IC50); PI3Kδ: 5 nM (IC50); mTOR: 12 nM (IC50)

References

[1] carnero a. novel inhibitors of the pi3k family. 2009.
[2] knight s d, adams n d, burgess j l, et al. discovery of gsk2126458, a highly potent inhibitor of pi3k and the mammalian target of rapamycin. acs medicinal chemistry letters, 2010, 1(1): 39-43.

5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione manufacturers

Career Henan Chemical Co
Product
5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione 958852-01-2
Price
US $1000.00-950.00/KG
Min. Order
1MG
Purity
98%
Supply Ability
100kg
Release date
2018-08-04

958852-01-2, 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedioneRelated Search:

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  • 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
  • GSK 1059615
  • (5Z)-5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidinedione
  • GSK 1059615;GSK-1059615
  • GSK 1059615 SodiuM Salt Hydrate
  • SK1059615
  • (5Z)-5-[[4-(4-pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidinedione sodium salt hydrate
  • GSK-615
  • GSK1059615;GSK 1059615; GSK-1059615
  • PI3K inhibitor GS1059615
  • CS-1726
  • CS-536
  • CS-1156
  • 2,4-Thiazolidinedione, 5-[[4-(4-pyridinyl)-6-quinolinyl]methylene]-, (5Z)-
  • 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione USP/EP/BP
  • GSK1059615, 10 mM in DMSO
  • 958852-01-2
  • Akt
  • mTOR
  • PI3K
  • Pharmaceuticals
  • Sulfur & Selenium Compounds
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals