BiochemProbe — Life Science Research Reagents

GLPG0187 free base · Synonyms: GLPG-0187 · GLPG 0187

GLPG0187 is a broad spectrum integrin receptor antagonist.

For research use only. Not for human or veterinary use.

Target Integrin
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

GLPG0187 structure

CAS No.: 1320346-97-1

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 550.00 BP-01867-250mg In stock Get quote
500 mg USD 880.00 BP-01867-500mg In stock Get quote
1 g USD 1,450.00 BP-01867-1g In stock Get quote
5 g Inquire BP-01867-5g Inquire Inquire

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Description

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.

Biological activity

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.

Identifiers

SMILES
COC1=CC=C(C=C1)S(=O)(=O)N[C@@H](CNC1=NC(C)=NC(N2CCC(CC2)C2=NC3=C(CCCN3)C=C2)=C1C)C(O)=O
InChIKey
CXHCNOMGODVIKB-VWLOTQADSA-N

Specifications

MW (average)
595.7130
Formula
C29H37N7O5S
CAS No.
1320346-97-1
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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]. Puzhong Lu, et al. Chemical screening identifies ROCK1 as a regulator of migrasome formation. Cell Discov. 2020 Aug 4;6(1):51.
[3]. 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.

Same target

Search Integrin

Same research area

Search Cancer