PF-8380 NEW
| Price | $38 | $83 | $137 |
| Package | 10mg | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: PF-8380 | CAS No.: 1144035-53-9 |
| Purity: 99.45% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | PF-8380 |
| Description | PF-8380 is an effective and orally available autotaxin inhibitor (IC50: 2.8 nM, in isolated enzyme assay; 101 nM, in the human whole blood). It modulates lysophosphatidic acid (LPA) levels in vivo/vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at the site of inflammation. |
| Cell Research | 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.(Only for Reference) |
| Kinase Assay | FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1]. |
| In vitro | Pre-treatment with PF-8380 before radiotherapy can inhibit radiation-induced angiogenesis in tumor endothelial cells and delay the growth and development of intracranial glioma tumors. In a rat air pouch inflammation model, PF8380 (30 mg/kg, p.o.) reduced inflammatory pain sensitivity and decreased LPA levels in plasma and inflamed tissues by more than 95% within 3 hours. |
| In vivo | PF-8380 inhibits autotoxin in rat substrates (IC50: 1.16 nM) and demonstrates inhibition in human whole blood with an IC50 of 101 nM after 2 hours of treatment [1]. Furthermore, PF-8380 suppresses autotoxin in GBM cells, subsequently reducing their invasion and migration capabilities while enhancing radiation sensitization. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : ＜1 mg/mL (insoluble or slightly soluble) |
| Keywords | inhibit | Phosphodiesterase (PDE) | PF 8380 | PF8380 | PF-8380 | Inhibitor |
| Inhibitors Related | Theophylline monohydrate | Diphylline | Acefylline | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Bioactive Lipid Compound Library | Anti-Metabolism Disease Compound Library | Anti-COVID-19 Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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