GSK-461364

Aha kemịkalụ:

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

Koodu Ọchịchọ:

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

Igodo InChi:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Okwu:

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

Solubility:Soluble na DMSO

Nchekwa:0 - 4 Celsius C maka obere oge (ụbọchị ruo izu), ma ọ bụ -20 Celsius maka ogologo oge (ọnwa)

Nkọwa:

Polo-dị ka kinases (Plks) bụ serine/threonine kinases nwere ọrụ dị mkpa na ịgba ígwè cell. GSK461364 bụ onye nwere ike, onye na-egbochi Plk1 (Ki = 2.2 nM). Ọ naghị adị irè megide Plk2 na Plk3 (Kis = 860 na 1,000 nM, n'otu n'otu) na opekata mpe 1,000-fold nhọrọ maka Plk1 n'elu otu panel nke 48 ndị ọzọ kinases. GSK461364 dose-dabere na-akwụsị ịnya igwe igwe n'ahịrị mkpụrụ ndụ kansa na-abawanye na, na oke doses, na-ebute apoptosis. Ọ dị ka ọ dị irè karị megide etuto erughi p53 ma nwee ike ịgafe mgbochi ụbụrụ ọbara. GSK461364 dị irè na vivo, na-ebute mgbochi uto tumor ma ọ bụ igbu oge uto na ụdị xenograft na ụmụ oke.

Ebumnuche: Plk1