G2171

GW843682X

≥98% (HPLC), solid

• Synonyme(s) : 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide, GW843682
• Formule empirique (notation de Hill) : C₂₂H₁₈F₃N₃O₄S
• CAS Number: 660868-91-7
• Poids moléculaire : 477.46
• Numéro MDL: MFCD09971143
• Code UNSPSC : 12352200
• ID de substance PubChem : 329799898
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥98% (HPLC)
• Forme: solid
• Couleur: off-white
• Solubilité: DMSO: >10 mg/mL
• Auteur: GlaxoSmithKline
• Température de stockage: 2-8°C
• Chaîne SMILES: COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC
• InChI: 1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)
• Clé InChI: JSKUWFIZUALZLX-UHFFFAOYSA-N

Description

Application

GW843682X has been used as a polo-like kinase-1 (PLK1) inhibitor:

• to study the influence of PLK1 inhibition on Wee1 (G2 check point kinase), cyclin-dependent protein kinase 1 (Cdc2)–Yp15, expression in melanoma cells
• to determine if PLK1 inhibition decreased the survival of hamartin and tuberin deficient cells
• to investigate if inhibitors of PLK1 and aurora kinases have a synergistic antimitotic impact in HeLa cells

Actions biochimiques/physiologiques

GW843682X is an anti-cancer compound. It can improve the ability of vincristine to promote growth arrest and apoptosis in leukemia cells. GW843682X is capable of disturbing the formation of spindles and terminate mitoses in lung adenocarcinoma cells.

GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor with nanomolar activity. It shows potent inhibition of proliferation of a wide variety of tumor cell lines.

Caractéristiques et avantages

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Équipement de protection individuelle: dust mask type N95 (US), Eyeshields, Gloves