ChemicalBook >?? ???? >??? ??>??? ??>???? ???>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

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ??? ???

?? ??:: 660868-91-7

???:: GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide

???(??):: GW843682;GW843682X;GW843682X (GW 843682X;GW843682X, 10 mM in DMSO;GW843682X GW843682X，S2880;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

CBNumber:: CB82090977

???:: C22H18F3N3O4S

??? ??:: 477.46

MOL ??:: 660868-91-7.mol

MSDS ??:: SDS

?? ?? 130

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ??

?? ?: 609.1±65.0 °C(Predicted)

??: 1.45±0.1 g/cm3(Predicted)

?? ??: 2-8°C

???: DMSO: >10mg/mL

??? ??: ??

??? ??: ??? ??

?? ?? (pKa): 15.03±0.50(Predicted)

??: ???

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

?? ? ?? ??
?? ? ???? ?? (GHS)

??? ??	Xi
?? ???? ??	36/37/38
?????	26-36/37
WGK ??	3
???? ???	11 - Combustible Solids

????(GHS):

?? ?:

Warning

??·?? ??:

??	??·?? ??	?? ??	??	?? ?	P- ??
H315	??? ??? ???	????? ?? ?????	?? 2	??	P264, P280, P302+P352, P321,P332+P313, P362
H319	?? ?? ??? ???	?? ? ?? ?? ??? ??	?? 2A	??	P264, P280, P305+P351+P338,P337+P313P
H335	?? ???? ??? ? ??	?? ???? ?? - 1? ??;???? ??	?? 3	??
H413	??? ??? ?? ????? ??? ??? ??	?? ????? ?? - ??	?? 4

??????:

P261	??·?·??·???·??·...·????? ??? ????.
P305+P351+P338	?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.

NFPA 704

	0
2		0

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide C??? ??, ??, ??

??

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.

??

GW843682X is a polo-like kinase-1 (PLK1) and polo-like kinase-3 (PLK3) inhibitor.

???? ??

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 ?? ?? ? ???

???

?? ??

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ?? ??

???( 130)?? ??

???	??	???	??	?? ?	??
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Aladdin Scientific		tp@aladdinsci.com	United States	52906	58

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide ?? ??:

GW 4064 GW-6604 Carbamic acid, N-[(5S)-5-[[(2R,3S)-3-(formylhydroxyamino)-2-(2-methylpropyl)-1-oxohexyl]amino]-6-oxo-6-(2-thiazolylamino)hexyl]-, phenylmethyl ester GW 627368X GW 6471 GW806742X Isopropyl-α-[2-methylhydrazino]-p-toluamide GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide

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