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G2171

Sigma-Aldrich

GW843682X

≥98% (HPLC), solid

Synonyme(s) :

5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide, GW843682

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About This Item

Formule empirique (notation de Hill):
C22H18F3N3O4S
Numéro CAS:
660868-91-7
Poids moléculaire :
477.46
Numéro MDL:
MFCD09971143
Code UNSPSC :
12352200
ID de substance PubChem :
329799898
Nomenclature NACRES :
NA.77

Pureté

≥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

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.

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

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Julio Vera et al.
Cellular signalling, 27(5), 951-960 (2015-02-17)
In the present report, the role of ATR-Chk1-Wee1 and ATM-Chk2-p53-p21 pathways in stress-induced cell cycle control is analysed in melanoma cells. Treatment of p53 wild-type melanoma cells with the genotoxic agent doxorubicin induces G2-M arrest, inhibitory phosphorylation of cell cycle
Qinyong Hu et al.
Anti-cancer agents in medicinal chemistry, 16(12), 1640-1645 (2016-05-21)
GW843682X is a publicly available anti-cancer compound by inhibiting Polo-like kinase. Previous studies revealed that GW843682X inhibited the proliferation of various tumor cell lines. In this study, the cytotoxic effect of GW843682X was investigated on cell proliferation, cell cycle and
Timothy J Lansing et al.
Molecular cancer therapeutics, 6(2), 450-459 (2007-02-03)
Polo-like kinase 1 (PLK1) plays key roles in the regulation of mitotic progression, including mitotic entry, spindle formation, chromosome segregation, and cytokinesis. PLK1 expression and activity are strongly linked to proliferating cells. Many studies have shown that PLK1 expression is
T Ikezoe et al.
Leukemia, 23(9), 1564-1576 (2009-05-08)
Polo-like kinase1 (PLK1) belongs to the family of serine/threonine kinases and plays an important role in centrosome maturation, bipolar spindle formation, and cytokinesis during mitosis. We found in this study that PLK1 was aberrantly highly expressed in a variety of
S A Watt et al.
Oncogene, 30(46), 4666-4677 (2011-05-24)
Identifying therapeutic targets for cancer treatment relies on consistent changes within particular types or sub-types of malignancy. The ability to define either consistent changes or sub-types of malignancy is often masked by tumor heterogeneity. To elucidate therapeutic targets in cutaneous
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