GLPG0187
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205842

CAS#: 1320346-97-1

Description: GLPG0187 is a small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity. Upon administration, GLPG0187 binds to and blocks the activity of 5 RGD-integrin receptor subtypes, including alphavbeta1, alphavbeta3, alphavbeta5, alphavbeta6 and alpha5beta1. This may result in the inhibition of endothelial cell-cell interactions and endothelial cell-matrix interactions, and the prevention of angiogenesis and metastasis in tumor cells expressing these integrin receptors. Integrin receptors are transmembrane glycoproteins expressed on the surface of tumor vessel endothelial cells and some types of cancer cells, and play a crucial role in endothelial cell adhesion and migration.


Price and Availability

Size
Price

100mg
USD 1450
1g
USD 3650
Size
Price

200mg
USD 1950
2g
USD 5950
Size
Price

500mg
USD 2850
5g
USD 9650

GLPG0187, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205842
Name: GLPG0187
CAS#: 1320346-97-1
Chemical Formula: C29H37N7O5S
Exact Mass: 595.2577
Molecular Weight: 595.719
Elemental Analysis: C, 58.47; H, 6.26; N, 16.46; O, 13.43; S, 5.38


Synonym: GLPG0187; GLPG 0187; GLPG-0187

IUPAC/Chemical Name: (S)-3-((2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl)pyrimidin-4-yl)amino)-2-((4-methoxyphenyl)sulfonamido)propanoic acid.

InChi Key: CXHCNOMGODVIKB-VWLOTQADSA-N

InChi Code: InChI=1S/C29H37N7O5S/c1-18-26(31-17-25(29(37)38)35-42(39,40)23-9-7-22(41-3)8-10-23)32-19(2)33-28(18)36-15-12-20(13-16-36)24-11-6-21-5-4-14-30-27(21)34-24/h6-11,20,25,35H,4-5,12-17H2,1-3H3,(H,30,34)(H,37,38)(H,31,32,33)/t25-/m0/s1

SMILES Code: 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


Technical Data

Appearance:
Solid powder

Purity:
>98%

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

GalapagosÂ’ candidate drug, GLPG0187, is an integrin receptor antagonist (IRA) that binds to six integrin receptors known to be present in many metastatic cancers, affording a unique anti-integrin profile. In animal studies, oral administration of GLPG0187 as a single agent has been shown to inhibit multiple processes involved in the spread and growth of metastatic tumors. GLPG0187 therefore offers a new approach to treat metastases, a severe complication of many cancers. In the first-in-human trial, GLPG0187 showed good safety and a promising biomarker profile in healthy volunteers. Based on these results, Galapagos initiated a Phase Ib study in March 2011. In this Phase Ib study, Galapagos plans to assess the safety and explore the preliminary efficacy of GLPG0187 in cancer patients. (source: http://www.glpg.com/index.php/randd/pipeline/glpg0187-cancer/).   
 
 
 


References

1: van der Horst G, van den Hoogen C, Buijs JT, Cheung H, Bloys H, Pelger RC, Lorenzon G, Heckmann B, Feyen J, Pujuguet P, Blanque R, Clément-Lacroix P, van der Pluijm G. 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. PubMed PMID: 21677875; PubMed Central PMCID: PMC3114245.