G2171
GW843682X
≥98% (HPLC), solid
别名:
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide, GW843682
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关于此项目
经验公式（希尔记法）:
C22H18F3N3O4S
化学文摘社编号:
分子量:
477.46
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
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
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 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.
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.
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.
存储类别
11 - Combustible Solids
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WGK 3
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