GSK-461364

Inoa Kimia:

(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

Code 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

Ki InChi:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Hua'ōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina)

wehewehe:

ʻO nā kinase like-polo (Plks) he serine/threonine kinases me nā kuleana koʻikoʻi i ke kaʻa uila. ʻO GSK461364 kahi mea hoʻopaneʻe ikaika o Plk1 (Ki = 2.2 nM). ʻAʻole maikaʻi loa ia e kūʻē iā Plk2 a me Plk3 (Kis = 860 a me 1,000 nM, kēlā me kēia) a ma ka liʻiliʻi he 1,000-paila koho no Plk1 ma luna o kahi papa o 48 mau kinase ʻē aʻe. ʻO GSK461364 e hoʻopau i ka hoʻopaʻa ʻana i ke kaʻa uila i nā laina cell cancer proliferating like ʻole a, ma nā kiʻekiʻe kiʻekiʻe, hoʻoulu i ka apoptosis. ʻIke ʻia ʻoi aku ka maikaʻi e kūʻē i nā maʻi maʻi p53-deficient a hiki ke hele i ka pale koko-lolo. He mea maikaʻi ʻo GSK461364 i loko o ka vivo, e hoʻoulu ai i ka ulu ʻana o ka tumo a i ʻole ka lohi o ka ulu ʻana i nā hiʻohiʻona xenograft i nā ʻiole.

Pahuhopu: Plk1