GSK-461364

Igama leMchiza:

(R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy) thiophene-2-carboxamide

Ikhowudi yoncumo:

O=C(C1=C(O[C@@H](C2=CC=CC=C2C(F)(F)F)C)C=C(N3C=NC4=CC=C(CN5CCN(C)CC5 )C=C34)S1)N

Ikhowudi ye-InChi:

InChI=1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31) 36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14, 16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1

Isitshixo se-InChi:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Igama elingundoqo:

GSK-461364, GSK461364, GSK 461364, GSK-461364A, GSK 461364A, GSK461364A, 929095-18-1

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga)

Inkcazo:

I-Polo-like kinases (Plks) yi-serine / threonine kinases eneendima eziphambili kwi-cell cycling. I-GSK461364 yinto enamandla, i-reversible inhibitor ye-Plk1 (Ki = 2.2 nM). Ayisebenzi kangako kwi-Plk2 kunye ne-Plk3 (i-Kis = 860 kunye ne-1,000 nM, ngokulandelanayo) kwaye ubuncinane i-1,000-fold selective ye-Plk1 phezu kwephaneli ye-48 yamanye ama-kinases. I-GSK461364 ixhomekeke kwidosi imisa ukukhwela ibhayisekile kweeseli kwiiseli zomhlaza ezandayo ezohlukeneyo kwaye, kwidosi ephezulu, ibangela i-apoptosis. Kubonakala ngathi isebenza ngakumbi ngokuchasene ne-p53-deficient tumors kwaye iyakwazi ukuwela umqobo wegazi-ubuchopho. I-GSK461364 iyasebenza kwi-vivo, ibangela inhibition yokukhula kwethumba okanye ukulibaziseka kokukhula kwiimodeli ze-xenograft kwiimpuku.

Ithagethi: Plk1