GSK-461364

Nomen chemicum:

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

SMILES Code:

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

InChi Code:

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

Keyword:

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

Solubilitas:Solutum in DMSO

Repono:0 - 4° C pro brevi termino (dies ad hebdomades), vel -20° C ad terminum longum (menses)

Descriptio:

Polo-kinases (Plks) sunt serinae/threoninae kinases cum muneribus clavis in cyclo cellularum. GSK461364 potens est, convertitur inhibitor Plk1 (Ki = 2.2 nM). Minus efficax est contra Plk2 et Plk3 (Kis = 860 et 1,000 nm, respective) et saltem 1,000-complex selectivum pro Plk1 super tabellam 48 aliarum kinasium. GSK461364 dosis dependenter claudit cellulam cyclicam in diversis lineis cancri multiplicando et, in dosibus superioribus, triggers apoptosin. Efficacior videtur contra tumores deficientium et impedimentum sanguinis cerebri transire potest. GSK461364 efficax est in vivo, inducendo tumorem inhibitionis vel augmenti incrementum morae in exemplaribus xenografis in muribus.

Target: Plk1