GSK-461364

Sunan Sinadari:

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

Lambar SMILES:

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

Lambar 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

Mabuɗin kalma:

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

Solubility:Mai narkewa a cikin DMSO

Ajiya:0 - 4 ° C na gajeren lokaci (kwanaki zuwa makonni), ko -20 ° C na dogon lokaci (watanni)

Bayani:

Kinases masu kama da Polo (Plks) sune kinases serine/threonine tare da manyan ayyuka a hawan keke. GSK461364 mai ƙarfi ne, mai hanawa na Plk1 (Ki = 2.2 nM). Yana da ƙarancin tasiri akan Plk2 da Plk3 (Kis = 860 da 1,000 nM, bi da bi) kuma aƙalla zaɓin 1,000-ninka don Plk1 akan panel na 48 sauran kinases. GSK461364 kashi-dogara yana dakatar da hawan keke a cikin layukan ƙwayoyin cuta masu yaduwa daban-daban kuma, a mafi girman allurai, yana haifar da apoptosis. Ya bayyana ya fi tasiri a kan ciwace-ciwacen p53 kuma yana iya ketare shingen kwakwalwar jini. GSK461364 yana da tasiri a cikin vivo, yana haifar da hana ci gaban tumo ko jinkirin girma a cikin xenograft a cikin mice.

manufa: Plk1