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

Element: inhibitor kinase like polo

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C-S » Chemicals » polo-like-kinase-inhibitor-iii-PX69945

Identification

Polo-like Kinase Inhibitor III

CAS:

660868-91-7

EINECS:

Molecular Formula:

C₂₂H₁₈F₃N₃O₄S

MDL:

MFCD09971143

SMILES:

COC1=C(C=C2C(=C1)N=CN2C3=CC(=C(S3)C(=O)N)OCC4=CC=CC=C4C(F)(F)F)OC

Synonym:

gw843682x ; 3-(2-(trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1h-benzo[d]imidazol-1-yl)thiophene-2-carboxamide ; 5-(5,6-dimethoxy-1h-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide ; polo-like kinase inhibitor iii ; gw843682 ; 5-(5,6-dimethoxy-1h-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ; gw843682, 5-(5,6-dimethoxy-1h-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ; 2-thiophenecarboxamide, 5-(5,6-dimethoxy-1h-benzimidazol-1-yl)-3 ; 2-thiophenecarboxamide,5-(5,6-dimethoxy-1h-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]- ; 5-(5,6-dimethoxy-1h-benzo[d]imidazol-1-yl)-3-((2-(trifluoromethyl)benzyl)oxy)thiophene-2-carboxamide

Description

Polo-like Kinase Inhibitor III (GW843682X) is a cell-permeable thiophene-benzimidazole compound that acts as a potent and reversible inhibitor against Plk (polo-like kinases) (K_i against Plk1/2/3/4 = 4.8, 3.8, 8.0, and 163 nM , respectively), while exhibiting little or much reduced activity against 39 other commonly studied kinases. Polo-like Kinase Inhibitor III preferentially inhibits the proliferation of a panel of 11 tumor cell lines (IC₅₀ ≤0.7 μM) over normal human diploid fibroblasts (IC₅₀ = 6.14 μM) in culture and is equally potent against the mdr-1-expressing MES-SA/DX5 and its parent non-drug resistant MES-SA uterine sarcoma cell line.

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