G2171

GW843682X

≥98% (HPLC), solid

• Synonym(s): 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide, GW843682
• Empirical Formula (Hill Notation): C₂₂H₁₈F₃N₃O₄S
• CAS Number: 660868-91-7
• Molecular Weight: 477.46
• MDL number: MFCD09971143
• UNSPSC Code: 12352200
• PubChem Substance ID: 329799898
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• color: off-white
• solubility: DMSO: >10 mg/mL
• originator: GlaxoSmithKline
• storage temp.: 2-8°C
• SMILES string: 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)
• InChI key: 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

Biochem/physiol Actions

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.

Features and Benefits

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves