GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide manufacturers
- GW843682X
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- $32.00
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2026-07-27
- CAS:660868-91-7
- Purity: 99.92%
- Supply Ability: 10g
- GW843682X
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- $1.00
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2020-01-13
- CAS:660868-91-7
- Min. Order: 1g
- Purity: 95-99%
- Supply Ability: 1ton
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| | GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Basic information |
| Product Name: | GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide | | Synonyms: | 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 | | CAS: | 660868-91-7 | | MF: | C22H18F3N3O4S | | MW: | 477.46 | | EINECS: | 200-258-5 | | Product Categories: | | | Mol File: | 660868-91-7.mol | ![GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Structure](CAS/GIF/660868-91-7.gif) |
| | GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Chemical Properties |
| 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 | | form | solid | | pka | 15.03±0.50(Predicted) | | color | off-white | | 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) | | InChIKey | JSKUWFIZUALZLX-UHFFFAOYSA-N | | SMILES | COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36/37 | | WGK Germany | 3 | | Storage Class | 11 - Combustible Solids |
| | GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Usage And Synthesis |
| 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 | | References | [1] TIMOTHY J LANSING. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1.[J]. Molecular Cancer Therapeutics, 2007, 6 2: 450-459. DOI: 10.1158/1535-7163.mct-06-0543
[2] T IKEZOE. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies[J]. Leukemia, 2009, 23 9: 1564-1576. DOI: 10.1038/leu.2009.94 |
| | GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide Preparation Products And Raw materials |
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