GLPG-0187

SKU: orb1226548

Description

GLPG-0187 (GLPG0187) is a highly potent, broad spectrum integrin receptor antagonist with IC50 of 1-10 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1; significantly inhibits angiogenesis both in vivo and in vitro, osteoclastogenesis in vitro, and bone loss in vivo; inhibits de novo formation and progression of bone and visceral metastases in prostate cancer and breast cancer mice models.Solid Tumors Phase 1 Clinical(In Vitro):In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors with IC50s of 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM for αvβ1, αvβ3, αvβ5, αvβ6,αvβ8, and α5β1. 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.(In Vivo):Blocking αv-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.

Key Properties

• CAS Number: 1320346-97-1
• MW: 595.713
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₇N₇O₅S
• 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
• Target: Integrin
• Solubility: DMSO: 15 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GLPG 0187 | GLPG0187

Quick Database Links

Gene Symbol

Integrin