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

Product Name: GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide
CAS No.: 660868-91-7
Chemical Name: GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide
Synonyms: GW843682;GW843682X;Polo-like Kinase Inhibitor III;GW843682X;GW 843682X;GW843682;GW-843682X;Polo-like Kinase Inhibitor III - CAS 660868-91-7 - Calbiochem;2-Thiophenecarboxamide, 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3;5-(5,6-dimethoxy-1-benzimidazolyl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide;5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide;3-(2-(Trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide;5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)-3-((2-(trifluoromethyl)benzyl)oxy)thiophene-2-carboxamide
CBNumber: CB82090977
Molecular Formula: C22H18F3N3O4S
Formula Weight: 477.46
MOL File: 660868-91-7.mol

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

Boiling point:: 609.1±65.0 °C(Predicted)
Density: 1.45±0.1 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: DMSO: >10mg/mL
pka: 15.03±0.50(Predicted)
form: solid
color: off-white

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Safety

Hazard Codes: Xi
Risk Statements: 36/37/38
Safety Statements: 26-36/37
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: G2171
Product name: GW843682X
Purity: ≥98% (HPLC), solid
Packaging: 1mg
Price: $178
Updated: 2024/03/01

Sigma-Aldrich

Product number: 528284
Product name: Polo-like Kinase Inhibitor III - CAS 660868-91-7 - Calbiochem
Packaging: 500μg
Price: $140
Updated: 2023/01/07

Cayman Chemical

Product number: 28759
Product name: GW843682X
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 28759
Product name: GW843682X
Packaging: 10mg
Price: $249
Updated: 2024/03/01

Sigma-Aldrich

Product number: G2171
Product name: GW843682X
Purity: ≥98% (HPLC), solid
Packaging: 5mg
Price: $567
Updated: 2024/03/01

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GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Chemical Properties,Usage,Production

Description

GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor. It selectively inhibits Plk1 and Plk3 (IC₅₀s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC₅₀s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC₅₀ = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC₅₀s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC₅₀ = 6.82 μM) or non-cancerous human diploid fibroblasts (HDFs; IC₅₀ = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC₅₀s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC₅₀s = <0.25-0.8 μM). GW843682X induces G₂/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.

Uses

GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor.

Definition

ChEBI: 5-(5,6-dimethoxy-1-benzimidazolyl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide is a member of (trifluoromethyl)benzenes.

Biological Activity

Selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC 50 values are 2.2 and 9.1 nM respectively). Displays > 100-fold selectivity over ~30 other kinases tested including cdk1 and cdk2. Inhibits proliferation of most tumor cells in vitro and is selective over normal diploid fibroblasts.

storage

Desiccate at +4°C

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Preparation Products And Raw materials

Raw materials

Preparation Products

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

China 92 India 1 Switzerland 1 The Netherlands 1 United Kingdom 1 United States 17 Global 113

3B Pharmachem (Wuhan) International Co.,Ltd.

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NCE Biomedical Co.,Ltd.

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Credit Asia Chemical Co., Ltd.

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LETOPHARM LIMITED

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View Lastest Price from GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide manufacturers

Career Henan Chemical Co

Product: GW843682X 660868-91-7
Price: US $1.00/g
Min. Order: 1g
Purity: 95-99%
Supply Ability: 1ton
Release date: 2020-01-10

660868-91-7, GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamideRelated Search:

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

GW843682X

3-(2-(Trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide

Polo-like Kinase Inhibitor III

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

5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide

GW843682

5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)-3-((2-(trifluoromethyl)benzyl)oxy)thiophene-2-carboxamide

2-Thiophenecarboxamide,5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-

2-Thiophenecarboxamide, 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3

GW843682X;GW 843682X;GW843682;GW-843682X

5-(5,6-dimethoxy-1-benzimidazolyl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide

Polo-like Kinase Inhibitor III - CAS 660868-91-7 - Calbiochem

660868-91-7

C22H18F3N3O4S