GLPG0187

Orukọ Kemikali:

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

KỌỌDỌ 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

Koodu 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

Bọtini InChi:

CXHCNOMGODVIKB-VWLOTQADSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

Ninu igbelewọn ipele-lile, GLPG0187 ṣe afihan yiyan fun ọpọlọpọ awọn olugba integrin RGD pẹlu IC50s ti 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM fun αvβ1, αvβ3, αvβ5, αvβ,6, αvβ8. GLPG0187 jẹ oludaniloju to lagbara ti isọdọtun egungun osteoclastic ati angiogenesis. Itọju pẹlu GLPG0187 iwọn lilo-igbẹkẹle ṣe alekun ipin E-cadherin/vimentin, fifun awọn sẹẹli naa ni epithelial diẹ sii, phenotype sessile. GLPG0187 iwọn lilo-igbẹkẹle n dinku iwọn aldehyde dehydrogenase giga ti awọn sẹẹli alakan pirositeti[1]. Awọn abajade itọju GLPG0187 ni yiyi sẹẹli ati iṣupọ. GLPG0187 ṣe afihan idinku iwọn-igbẹkẹle pataki idinku ninu ijira sẹẹli tumo. GLPG0187 ni gbogbo awọn ifọkansi ni pataki dinku ilọsiwaju sẹẹli [2].

Àfojúsùn: αvβ1