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GLPG-0187

CAT: 0013-GTR19163854-01Size: 1 gDry Ice: NoHazardous: No
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CAT#:0013-GTR19163854-01Size:1 g
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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.
CAS Number
1320346-97-1
Product Name Alternative
GLPG 0187 | GLPG0187
Purity
>98% (HPLC)
Solubility
DMSO: 15 mg/mL
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
Molecular Formula
C29H37N7O5S
Molecular Weight
595.713
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
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]-

Chemical Information

Glpg-0187

GLPG0187 has been used in trials studying the treatment of Solid Tumors.

CAS Number1320346-97-1
PubChem CID53340771
IUPAC Name(2S)-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)sulfonylamino]propanoic acid
Molecular FormulaC29H37N7O5S
Molecular Weight595.7
XLogP4.5
Topological Polar Surface Area167
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count12
Rotatable Bond Count10
Heavy Atom Count42
Formal Charge0
Complexity983
SMILES
CC1=C(N=C(N=C1N2CCC(CC2)C3=NC4=C(CCCN4)C=C3)C)NC[C@@H](C(=O)O)NS(=O)(=O)C5=CC=C(C=C5)OC
InChI
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
InChIKey
CXHCNOMGODVIKB-VWLOTQADSA-N
Chemical Structure
2D Structure
2D structure of Glpg-0187
CAS: 1320346-97-1
CID: 53340771
Formula: C29H37N7O5S
MW: 595.7
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight595.7
XLogP34.5
Hydrogen Bond Donor Count4
Hydrogen Bond Acceptor Count12
Rotatable Bond Count10
Exact Mass595.25768848
Monoisotopic Mass595.25768848
Topological Polar Surface Area167 Ų
Heavy Atom Count42
Formal Charge0
Complexity983
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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