SML0083

GSK 1059615 sodium salt hydrate

• Synonym(s): (5Z)-5-[[4-(4-pyridinyl)-6-quinolinyl]methylene]-2,4-thiazolidinedione sodium salt hydrate
• Empirical Formula (Hill Notation): C₁₈H₁₀N₃O₂S·Na · xH₂O
• CAS Number: 1356195-42-0
• Molecular Weight: 355.35 (anhydrous basis)
• UNSPSC Code: 12352203
• PubChem Substance ID: 329825144
• NACRES: NA.44

Properties

• form: powder
• Quality Level: 100
• color: yellow
• solubility: H₂O: ≥8 mg/mL
• originator: GlaxoSmithKline
• storage temp.: 2-8°C
• SMILES string: O.[Na+].O=C1[N-]C(=O)C(\S1)=C\c2ccc3nccc(-c4ccncc4)c3c2
• InChI: 1S/C18H11N3O2S.Na.H2O/c22-17-16(24-18(23)21-17)10-11-1-2-15-14(9-11)13(5-8-20-15)12-3-6-19-7-4-12;;/h1-10H,(H,21,22,23);;1H2/q;+1;/p-1/b16-10-;;
• InChI key: KKSRFFGUIONCPS-FLPKAINGSA-M

Description

Biochem/physiol Actions

GSK 1059615 is a phosphatidylinositol-3-kinases (PI3K) inhibitor. GSK 1059615 inhibits proliferation of breast cancer BT474 cells via four different mechanisms that include retinoblastoma 1 (RB1)-mediated cell cycle arrest, elevated forkhead box protein O1 (FOXO) signaling, deduced MYC and transferrin receptor (TFRC) signaling and decreased cellular metabolism. Additionally, GSK 1059615 can suppress cell proliferation by decreasing mitogen-activated protein kinase (MAPK) signaling and imparts sensitivity to phosphoinositide 3-kinase (PI3K) inhibitor in cells resistant to the protein kinase B or AKT inhibitor. GSK 1059615 functions as a druggable target to reduce radiation-induced apoptosis in NCCIT cells. GSK 1059615 has entered clinical trial in patients with solid tumors or lymphoma and refractory malignancies.

GSK 1059615 is a potent inhibitor of PI3 Kinase. (IC₅₀ = 2 nM)

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Disclaimer

Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable