An αν integrin receptor antagonist (IC50s = 1.2-3.7 nM); inhibits hallmarks of bone marrow invasion in metastatic prostate cancer in vitro and in vivo; reduces EMT and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth; induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells

GLPG0187 – 10 mg

Brand:
Cayman
CAS:
1320346-97-1
Storage:
-20
UN-No:
Non-Hazardous - /

GLPG0187 is a nonpeptide antagonist of αν integrin receptors (IC50s = 1.2-3.7 nM).{38088} It inhibits osteoclastogenesis, bone resorption, and angiogenesis in vitro and in vivo in mice, which are all hallmarks of bone marrow invasion in metastatic prostate cancer. GLPG0187 reduces epithelial-mesenchymal transition (EMT) and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth. GLPG0187 also induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells.{38089} Formulations containing GLPG0187 are being tested in Phase I clinical trials for the treatment of high-grade gliomas and other advanced solid malignancies.{38090}  

 

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Description

An αν integrin receptor antagonist (IC50s = 1.2-3.7 nM); inhibits hallmarks of bone marrow invasion in metastatic prostate cancer in vitro and in vivo; reduces EMT and migration of PC-3M-Pro4/luc cells in a dose-dependent manner without inhibiting cell growth; induces detachment and necrosis of GL-261 and SMA-560 murine glioma cells,

Formal name: 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]-L-alanine

Synonyms: 

Molecular weight: 595.7

CAS: 1320346-97-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death|Necrosis||Research Area|Cancer|Cell Migration & Metastasis

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