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GLPG0187

Cat. No. M5241
GLPG0187  Structure
Size Price Availability Quantity
10mM*1mL USD 480  USD480 In stock
1mg USD 133  USD133 In stock
5mg USD 366  USD366 In stock
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Quality Control & Documentation
Biological Activity

GLPG0187 treatment significantly (p < 0.05) reduced PC3 cell number within the metatarsal in vivo and reduced migration (p < 0.05) and proliferation (p < 0.05) but not cell viability in vitro. This new model allows evaluation of the early events of tumour-cell homing and localisation to the bone microenvironment, in addition to determining responses to therapeutic interventions.

Customer Product Validations & Biological Datas
Source Int J Cancer (2015). Figure 3. GLPG0187
Method cell viability, proliferation, migration assay
Cell Lines PC3 cell
Concentrations 50 ng/ml
Incubation Time 96 hr
Results GLPG0187 significantly (p<0.05) reduced the number of tumour cells present in the implanted metatarsal from day 17 on ward
Chemical Information
Molecular Weight 595.71
Formula C29H37N7O5S
CAS Number 1320346-97-1
Solubility (25°C) 10mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Li Y, et al, Breast Cancer Res. Genetic depletion and pharmacological targeting of αv integrin in breast cancer cells impairs metastasis in zebrafish and mouse xenograft models.

[2] Reeves KJ, et al. Int J Cancer. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187.

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