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
- Molecular Weight:
- 477.46
- MOL File:
- 660868-91-7.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/9/4 15:51:00
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H315-H319-H335-H413 | |||||||||
Precautionary statements | P261-P305+P351+P338 | |||||||||
Hazard Codes | Xi | |||||||||
Risk Statements | 36/37/38 | |||||||||
Safety Statements | 26-36/37 | |||||||||
WGK Germany | 3 | |||||||||
NFPA 704 |
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GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide price More Price(3)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | G2171 | GW843682X ≥98% (HPLC), solid | 660868-91-7 | 1MG | ₹16962.78 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | G2171 | GW843682X ≥98% (HPLC), solid | 660868-91-7 | 5MG | ₹68414 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | 528284 | Polo-like Kinase Inhibitor III - CAS 660868-91-7 - Calbiochem The Polo-like Kinase Inhibitor III, also referenced under CAS 660868-91-7, controls the biological activity of Polo-like Kinase. This small molecule/i | 660868-91-7 | 500μG | ₹9490 | 2022-06-14 | Buy |
GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Chemical Properties,Uses,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.
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.
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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CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49392 | 58 | Inquiry |
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GIHI CHEMICALS CO.,LIMITED | +8618058761490 | China | 50003 | 58 | Inquiry |
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