In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
PF-8380 is a potent autotaxin (ATX) inhibitor with an IC50 of 2.8 nM in an in vitro enzyme assay.
Targets
Autotaxin (Cell-free assay)
2.8 nM
In vitro
PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM with FS-3 substrate. In human whole blood incubated with this compound for 2 h autotaxin was inhibited with an IC50 of 101 nM.Inhibition of autotaxin by this chemical leads to decreased invasion, migration and enhanced radiosensitization of GBM cells. Radiation-induced activation of Akt is abrogated by inhibition of ATX. Furthermore, inhibition of ATX leads to diminished tumour vascularity and delayed tumour growth.
In Vivo
Pre-treatment with PF-8380 prior to irradiation inhibited radiation-induced angiogenesis of tumour vascular endothelial cells and delayed progression of glioma tumour growth in vivo. Oral administration of 30 mg/kg of this compound reduces inflammatory hyperalgesia in a rat air pouch model, exhibiting >95% reduction of LPA levels in both plasma and inflammatory site tissue within 3 hours.
GL261 or U87-MG cells are plated in triplicate onto 6 cm plates and allowed to grow to 70% confluence. The semi-confluent cell layer is scratched with a sterile 200 μL pipette tip to create a scratch devoid of cells and plates are washed once with PBS to remove non-adherent cells and debris. For radiosensitization drug studies, cells are treated with 1 μM PF-8380 or DMSO for 45 min prior to irradiation with 4 Gy, and then incubated at 37°C in 5% CO2. Control plates are monitored for cell migration (20–24 h). Cells are fixed with 70% ethanol and stained with 1% methylene blue. To quantify migration, cells in three randomly selected high power fields (HPFs) in the scratched area are counted and normalized for surrounding cell density.
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
