GLPG0187

Ingoa matū:

(S)-3-((2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl)pirimidin-4- yl)amino)-2-((4-methoxyphenyl)sulfonamido)waikawa propanoic

Waehere SMILES:

O=C(O)[C@H](CNC1=NC(C)=NC(N2CCC(C3=NC4=C(CCCN4)C=C3)CC2)=C1C)NS(=O)(C5=CC= C(OC)C=C5)=O

Waehere InChi:

InChI=1S/C29H37N7O5S/c1-18-26(31-17-25(29(37)38)35-42(39,40)23-9-7-22(41-3)8-10-23) 32-19(2)33-28(18)36-15-12-20(13-16-36)24-11-6-21-5-4-14-30-27(21)34-24/ h6-11,20,25,35H,4-5,12-17H2,1-3H3,(H,30,34)(H,37,38)(H,31,32,33)/t25-/m0 /s1

Kī InChi:

CXHCNOMGODVIKB-VWLOTQADSA-N

Kupumatua:

GLPG0187, GLPG-0187, GLPG 0187, 1320346-97-1

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

I roto i te whakamatautau-waahanga totoka, ka whakaatu a GLPG0187 i te whiriwhiringa mo te maha o nga kaiwhakawhiwhi RGD integrin me nga IC50 o 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM mo te αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, me te αvβ8. Ko te GLPG0187 he aukati kaha o te resorption wheua osteoclastic me te angiogenesis. Ko te maimoatanga me te GLPG0187 te horopeta-e whakawhirinaki ana ki te whakanui ake i te ōwehenga E-cadherin/vimentin, ka nui ake te epithelial, sessile phenotype o nga pūtau. GLPG0187 horopeta-ti'aturi whakaiti i te rahi o te aldehyde dehydrogenase subpopulation teitei o ngā pūtau mate pukupuku prostate[1]. Ko te maimoatanga GLPG0187 e hua ana i te whakaawhiwhinga o te pūtau me te kopiri. Ko te GLPG0187 e whakaatu ana i te whakahekenga nui o te horopeta-ti'aturi i roto i te hekenga pūtau puku. Ko te GLPG0187 i nga kohinga katoa ka tino whakaiti i te tipu o nga pūtau [2].

Whāinga: αvβ1