GSK-461364
Tsatanetsatane wa Zamalonda
Zolemba Zamalonda
| Paketi Kukula | Kupezeka | Mtengo (USD) |
| 100 mg | Zilipo | 400 |
| 500 mg | Zilipo | 1400 |
| Makulidwe Enanso | Pezani Mawu | Pezani Mawu |
Dzina la Chemical:
(R) -5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy) thiophene-2-carboxamide
SMILES Kodi:
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 kodi:
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
Mawu ofunika:
GSK-461364, GSK461364, GSK 461364, GSK-461364A, GSK 461364A, GSK461364A, 929095-18-1
Kusungunuka:Zosungunuka mu DMSO
Posungira:0 - 4 ° C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 ° C kwa nthawi yaitali (miyezi)
Kufotokozera:
Polo-ngati kinase (Plks) ndi serine/threonine kinases omwe ali ndi maudindo ofunikira pakuyendetsa ma cell. GSK461364 ndi choletsa champhamvu, chosinthika cha Plk1 (Ki = 2.2 nM). Ndiwopanda mphamvu polimbana ndi Plk2 ndi Plk3 (Kis = 860 ndi 1,000 nM, motsatira) komanso kusankha ka 1,000 kwa Plk1 pagulu la kinase 48. GSK461364 modalira mlingo imayimitsa kuyendetsa njinga m'maselo a khansa omwe akuchulukirachulukira ndipo, pamilingo yayikulu, imayambitsa apoptosis. Zikuwoneka kuti ndizothandiza kwambiri polimbana ndi zotupa zopanda p53 ndipo zimatha kuwoloka chotchinga chamagazi-muubongo. GSK461364 imagwira ntchito mu vivo, kupangitsa kuletsa kukula kwa chotupa kapena kuchedwa kwakukula mumitundu ya xenograft mu mbewa.
Cholinga: Plk1
