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.
|Source||Int J Cancer (2015). Figure 3. GLPG0187|
|Method||cell viability, proliferation, migration assay|
|Cell Lines||PC3 cell|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10mM in DMSO|
Genetic depletion and pharmacological targeting of αv integrin in breast cancer cells impairs metastasis in zebrafish and mouse xenograft models.
Li Y, et al, Breast Cancer Res. 2015 Feb 25;17:28. PMID: 25849225.
Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187.
Reeves KJ, et al. Int J Cancer. 2015 Apr 1;136(7):1731-40. PMID: 25156971.
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