A reversible

GW843682X – 1 mg

Brand:
Cayman
CAS:
660868-91-7
Storage:
-20
UN-No:
Non-Hazardous - /

GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} 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 = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}  

 

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SKU: 28759 - 1 mg Category:

Description

A reversible, cell-permeable PLK inhibitor; selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over more than 30 other kinases in a cell-free assay; inhibits Plk1 activity in vitro in HeLa cells using a chimeric Plk1 reporter assay (IC50 = 0.14 μM); 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); 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); inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner

Formal name: 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide

Synonyms: 

Molecular weight: 477.5

CAS: 660868-91-7

Purity: ≥98%

Formulation: A crystalline solid

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