GSK-461364

Magaca Kiimikada:

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

Koodhka dhoola cadeynta:

O=C(C1=C(O[C@@H](C2=CC=CC=C2C(F)(F)F)C=C(N3C=NC4=CC=C(CN5CCN(C)CC5 )C=C34)S1)N

Koodhka 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

Furaha InChi:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo)

Sharaxaad:

Kinases-ka Polo (Plks) waa serine/threonine kinases oo leh door muhiim ah baaskiil wadida unugga. GSK461364 waa ka hortag awood leh, celin kara ee Plk1 (Ki = 2.2 nM). Way yar tahay waxtarka marka loo eego Plk2 iyo Plk3 (Kis = 860 iyo 1,000 nM, siday u kala horreeyaan) iyo ugu yaraan 1,000-laab oo loo xushay Plk1 oo ka sarreeya guddi ka kooban 48 kinases kale. GSK461364 qiyaasta-ku-tiirsanaanta waxay joojisaa baaskiil-waynta unugga ee khadadka unugyada kansarka ee kala duwan, iyo, qiyaasta sare, waxay kicisaa apoptosis. Waxa ay u muuqataa in ay aad uga waxtar badan tahay burooyinka p53-yar oo awood u leh in ay ka gudubto xannibaadda dhiigga-maskaxda. GSK461364 waa wax ku ool ah gudaha Vivo, taasoo keenta xakameynta koritaanka burooyinka ama dib u dhigista koritaanka moodooyinka xenograft ee jiirarka.

Ujeedka: Plk1