GSK-461364

Lebitso la lik'hemik'hale:

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

SMILES Khouto:

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

Khoutu ea 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

InChi Key:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Keyword:

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

Sollubility:E qhibiliha ka DMSO

Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli)

Tlhaloso:

Polo-like kinases (Plks) ke serine/threonine kinases e nang le likarolo tsa bohlokoa ho baesekele ea lisele. GSK461364 ke inhibitor e matla, e fetolehang ea Plk1 (Ki = 2.2 nM). Ha e sebetse hantle khahlanong le Plk2 le Plk3 (Kis = 860 le 1,000 nM, ka ho latellana) 'me bonyane e khethoa ka makhetlo a 1,000 bakeng sa Plk1 holim'a phanele ea 48 kinase. GSK461364 e itšetlehile ka tekanyo ea litekanyetso e emisa ho palama libaesekele mecheng e fapaneng ea lisele tsa mofetše, 'me ka litekanyetso tse phahameng, e baka apoptosis. E bonahala e sebetsa haholoanyane khahlanong le lihlahala tse haelloang ke p53 'me e khona ho tšela mokoallo oa mali-boko. GSK461364 e sebetsa hantle ho vivo, e baka thibelo ea kholo ea tumor kapa ho lieha ho hola mefuteng ea xenograft ho litoeba.

Sepheo: Plk1