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G2171

GW843682X

Name: GW843682X
Brand: SIGMA

≥98% (HPLC), solid

Synonym(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

Empirical Formula (Hill Notation):

C₂₂H₁₈F₃N₃O₄S

CAS Number:

660868-91-7

Molecular Weight:

477.46

NACRES:

NA.77

PubChem Substance ID:

329799898

UNSPSC Code:

12352200

MDL number:

MFCD09971143

Assay:

≥98% (HPLC)

Form:

solid

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Properties

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 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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves

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