DC Chemicals Limited
China
Product Name: GLPG0187
Price: $1400.0/250mg $2700.0/1g $800.0/100mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

1320346-97-1

1320346-97-1 structure

1320346-97-1 structure

Name: GLPG 0187
Chemical Name: GLPG0187
CAS Number: 1320346-97-1
Molecular Formula: C₂₉H₃₇N₇O₅S
Molecular Weight: 595.713
Catalog: Signaling Pathways Cytoskeleton Integrin
Create Date: 2018-01-27 13:25:23
Modify Date: 2024-01-21 17:15:17
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.

Name	GLPG0187
Synonyms	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 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]-

Description	GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
Related Catalog	Signaling Pathways >> Cytoskeleton >> Integrin Research Areas >> Cancer
Target	IC50: 1.3 nM (αvβ1)[1]
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[1]. 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[2].
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[1].
Cell Assay	Tumour cell proliferation is determined using the MTS assay. PC3 cells are seeded at 10,000 cells/well in 96 well plates containing either GLPG0187 (0.5, 5, or 50 ng/mL), vehicle or media control, then cultured in 100 µL medium for 24 hr. Cell proliferation is analysed using 20 µL MTS dye incubated for 3 hr at 37°C in the dark. Absorbance from each well (6/treatment) is quantified at 490 nm and the mean fluorescence calculated. The assay is repeated at 48, 72 and 96 hr, on three independent occasions[2].
Animal Admin	Mice: The effect of GLPG0187 on bone loss is evaluated in 3-month-old castrated male mice after 4 weeks of treatment with dosing starting immediately after castration (preventive protocol). Two different modes of administration are used: either subcutaneous twice daily with 10, 30, or 100 mg/kg of GLPG0187, either oral, twice daily with 30, 100, or 300 mg/kg of GLPG0187[1].
References	[1]. van der Horst G, et al. Targeting of α(v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia. 2011 Jun;13(6):516-25. [2]. Reeves KJ, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187. Int J Cancer. 2015 Apr 1;136(7):1731-40.

Density	1.3±0.1 g/cm3
Boiling Point	872.8±75.0 °C at 760 mmHg
Molecular Formula	C₂₉H₃₇N₇O₅S
Molecular Weight	595.713
Flash Point	481.6±37.1 °C
Exact Mass	595.257690
LogP	4.94
Vapour Pressure	0.0±0.3 mmHg at 25°C
Index of Refraction	1.621
Storage condition	2-8℃