I-GSK-461364

Igama Lekhemikhali:

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

Ikhodi ye-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

Ikhodi ye-InChi:

I-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

I-InChi Key:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga)

Incazelo:

I-Polo-like kinases (i-Plks) i-serine/threonine kinases enendima ebalulekile ekujikelezeni kwamaseli. I-GSK461364 iyisivimbi esinamandla, esibuyiseleka emuva se-Plk1 (Ki = 2.2 nM). Ayisebenzi kahle uma iqhathaniswa ne-Plk2 ne-Plk3 (Kis = 860 kanye ne-1,000 nM, ngokulandelanayo) futhi okungenani ikhethwa ngokuphindwe ka-1,000 ku-Plk1 phezu kwephaneli yamanye ama-kinases angu-48. I-GSK461364 ngokuncika kumthamo imisa ukuhamba kwamabhayisikili emigqeni yamaseli omdlavuza andayo ahlukahlukene futhi, ngemithamo ephezulu, icuphe i-apoptosis. Kubonakala kusebenza kakhulu ngokumelene namathumba angenayo i-p53 futhi iyakwazi ukweqa umgoqo wegazi nobuchopho. I-GSK461364 iyasebenza ku-vivo, idala ukuvimbela ukukhula kwesimila noma ukubambezeleka kokukhula kumamodeli we-xenograft kumagundane.

Ithagethi: Plk1