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

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

Product Name:	5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
Synonyms:	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
CAS:	958852-01-2
MF:	C18H11N3O2S
MW:	333.36
EINECS:
Product Categories:	Akt;mTOR;Aromatics;Pharmaceuticals;Sulfur & Selenium Compounds;PI3K;Heterocycles;Inhibitors;Intermediates & Fine Chemicals
Mol File:	958852-01-2.mol

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

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

Safety Information

WGK Germany

MSDS Information

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

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

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

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