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
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
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.
N-Bromosuccinimide Price
- Product number
- G2171
- Product name
- GW843682X
- Purity
- ≥98% (HPLC), solid
- Packaging
- 1mg
- Price
- $178
- Updated
- 2024/03/01
- Product number
- 528284
- Product name
- Polo-like Kinase Inhibitor III - CAS 660868-91-7 - Calbiochem
- Packaging
- 500μg
- Price
- $140
- Updated
- 2023/01/07
- Product number
- 28759
- Product name
- GW843682X
- Packaging
- 1mg
- Price
- $57
- Updated
- 2024/03/01
- Product number
- 28759
- Product name
- GW843682X
- Packaging
- 10mg
- Price
- $249
- Updated
- 2024/03/01
- Product number
- G2171
- Product name
- GW843682X
- Purity
- ≥98% (HPLC), solid
- Packaging
- 5mg
- Price
- $567
- Updated
- 2024/03/01
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
GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Suppliers
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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
- Product
- GW843682X 660868-91-7
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 95-99%
- Supply Ability
- 1ton
- Release date
- 2020-01-10