GSK-461364

Orukọ Kemikali:

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

KỌỌDỌ 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

Koodu 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

Bọtini InChi:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu)

Apejuwe:

Polo-like kinases (Plks) jẹ serine/threonine kinases pẹlu awọn ipa pataki ninu gigun kẹkẹ sẹẹli. GSK461364 jẹ apaniyan ti o lagbara, iparọpo ti Plk1 (Ki = 2.2 nM). Ko munadoko lodi si Plk2 ati Plk3 (Kis = 860 ati 1,000 nM, lẹsẹsẹ) ati pe o kere ju 1,000-agbo yiyan fun Plk1 lori nronu 48 miiran kinases. GSK461364 iwọn lilo-igbẹkẹle da duro gigun kẹkẹ sẹẹli ni oniruuru awọn laini sẹẹli alakan ti o pọ si ati, ni awọn iwọn ti o ga julọ, nfa apoptosis. O dabi pe o munadoko diẹ sii lodi si awọn èèmọ aipe p53 ati pe o ni anfani lati kọja idena-ọpọlọ ẹjẹ. GSK461364 jẹ doko ni vivo, ti nfa idinamọ idagbasoke tumo tabi idaduro idagbasoke ni awọn awoṣe xenograft ninu awọn eku.

afojusun: Plk1