1320346-97-1
基本信息
GLPG0187, 一种广谱的INTEGRIN受体拮抗剂,具有抗肿瘤活性
GLPG0187
GLPG 0187
GLPG-0187
GLPG0187, 98%, a broad spectrum integrin receptor antagonist with antitumor activity
L-Alanine, 3-[[2,5-dimethyl-6-[4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)-1-piperidinyl]-4-pyrimidinyl]amino]-N-[(4-methoxyphenyl)sulfonyl]-
(S)-3-(2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl)pyrimidin-4-ylamino)-2-(4-methoxyphenylsulfonamido)propanoic acid
物理化学性质
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/04/30 | HY-100506 | GLPG0187, 一种广谱的INTEGRIN受体拮抗剂,具有抗肿瘤活性 GLPG0187 | 1320346-97-1 | 5mg | 3300元 |
2024/04/30 | HY-100506 | GLPG0187, 一种广谱的INTEGRIN受体拮抗剂,具有抗肿瘤活性 GLPG0187 | 1320346-97-1 | 10mM * 1mLin DMSO | 4325元 |
2024/04/30 | HY-100506 | GLPG0187, 一种广谱的INTEGRIN受体拮抗剂,具有抗肿瘤活性 GLPG0187 | 1320346-97-1 | 10mg | 4500元 |
常见问题列表
IC50: 1.3 nM (α v β 1 )
In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors with IC 50 s of 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM for α v β 1 , α v β 3 , α v β 5 , α v β 6 ,α v β 8 , and α 5 β 1 . GLPG0187 is a potent inhibitor of osteoclastic bone resorption and angiogenesis. Treatment with GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio, rendering the cells a more epithelial, sessile phenotype. GLPG0187 dose-dependently diminishes the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells. GLPG0187 treatment results in cell rounding and clumping. GLPG0187 demonstrates a dose-dependent significant reduction in tumour cell migration. GLPG0187 at all concentrations significantly reduces cell proliferation.
Blocking α v -integrins by GLPG0187 markedly reduces their metastatic tumor growth. Bone tumor burden is significantly lower and the number of bone metastases/mouse is significantly inhibited. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited.