GSK-461364

Non Chimik:

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

Kòd 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

Kòd 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 kle:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Mot:

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

Solibilite:Soluble nan DMSO

Depo:0 - 4 ° C pou kout tèm (jou a semèn), oswa -20 ° C pou tèm long (mwa)

Deskripsyon:

Polo kinases (Plks) se serine/threonine kinases ak wòl kle nan sèlil cycling. GSK461364 se yon inibitè ki pisan, revèsib nan Plk1 (Ki = 2.2 nM). Li mwens efikas kont Plk2 ak Plk3 (Kis = 860 ak 1,000 nM, respektivman) ak omwen 1,000-pliye selektif pou Plk1 sou yon panèl 48 lòt kinaz. GSK461364 depann de dòz la sispann sikilasyon selilè nan divès liy selil kansè nan pwopagasyon epi, nan dòz ki pi wo, deklanche apoptoz. Li parèt pi efikas kont timè p53-defisyan epi li kapab travèse baryè san-sèvo. GSK461364 efikas nan vivo, pwovoke anpèchman kwasans timè oswa reta kwasans nan modèl xenograft nan sourit.

Sib: Plk1