5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
Synonym(s):(5Z)-5-[[4-(4-pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidinedione sodium salt hydrate
- CAS NO.:958852-01-2
- Empirical Formula: C18H11N3O2S
- Molecular Weight: 333.36
- MDL number: MFCD18074517
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-01 18:44:47
What is 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione?
The Uses of 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
GSK 1059615 is a potent inhibitor of PI 3-kinase α (PI3Kα). GSK 1059615 inhibits proliferation in BT474 cells and attenuates MAPK signaling.
The Uses of 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
GSK 1059615 is a potent inhibitor of PI 3-kinase and FRAP (mTOR).
What are the applications of Application
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.
Properties of 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
Melting point: | >290°C (dec.) |
storage temp. | Store at +4°C |
solubility | H2O: ≥8mg/mL |
form | powder |
color | yellow |
Safety information for 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for 5-[[4-(4-Pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidenedione
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