GSK-461364

Igoa vaila'au:

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

SMILES Code:

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

InChi Code:

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

InChi Key:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

upu autu:

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

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), po'o le -20°C mo taimi uumi (masina)

Fa'amatalaga:

Polo-pei kinases (Plks) o serine / threonine kinases ma matafaioi autu i le uila uila. GSK461364 o se faʻamalosi malosi, toe faʻaaogaina o le Plk1 (Ki = 2.2 nM). E itiiti le aoga e faasaga i le Plk2 ma le Plk3 (Kis = 860 ma le 1,000 nM, fa'asologa) ma le itiiti ifo i le 1,000-filifili filifilia mo Plk1 i luga o se laulau o 48 isi kinases. GSK461364 fua fa'atatau-fa'alagolago e taofi le uila uila i le tele o laina sela o le kanesa fa'ateleina ma, i le maualuga o tui, fa'aoso apoptosis. E foliga mai e sili atu le aoga e faasaga i le p53-le atoatoa tuma ma mafai ona laasia le pa puipui toto-faiai. GSK461364 e aoga i vivo, faʻaosoina le tuputupu aʻe o le tumo poʻo le tuai o le tuputupu aʻe i faʻataʻitaʻiga xenograft i isumu.

Sini: Plk1