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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H21Cl2N3O5 |
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分子量 | 478.33 | CAS No. | 1144035-53-9 | |
Solubility (25°C)* | 体外 | DMSO | 95 mg/mL (198.6 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <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. |
製品説明 | PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay. |
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in vitro | PF-8380 inhibits rat autotaxin with an IC50 of 1.16 nM with FS-3 substrate. In human whole blood incubated with compound for 2 h autotaxin was inhibited with an IC50 of 101 nM[1].Inhibition of autotaxin by PF-8380 leads to decreased invasion, migtation and enhanced radiosensitization of GBM cells. Radiation-induced activation of Akt is abrogated by inhibition of ATX. Furthermore, inhibition of ATX leads to diminished tumor vascularity and delayed tumor growth[2]. |
in vivo | Pre-treatment with PF-8380 prior to irradiation inhibited radiation-induced angiogenesis of tumor vascular endothelial cells and delayed progression of glioma tumor growth in vivo[2]. Oral administration of 30 mg/kg PF8380 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[1]. |
細胞アッセイ | 細胞株 | Mouse GL261 and Human U87-MG cells |
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濃度 | 1 μM | |
反応時間 | 45 min | |
実験の流れ | 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. | |
動物実験 | 動物モデル | Male Lewis rats |
投薬量 | 1, 3, 10, 30, and 100 mg/kg | |
投与方法 | by oral gavage |
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Autotaxin suppresses cytotoxic T cells via LPAR5 to promote anti-PD-1 resistance in non-small cell lung cancer [ J Clin Invest, 2023, 133(17)e163128] | PubMed: 37655662 |
Autotaxin suppresses cytotoxic T cells via LPAR5 to promote anti-PD-1 resistance in non-small cell lung cancer [ J Clin Invest, 2023, 133(17)e163128] | PubMed: 37655662 |
EMT activates exocytotic Rabs to coordinate invasion and immunosuppression in lung cancer [ Proc Natl Acad Sci U S A, 2023, 120(28):e2220276120] | PubMed: 37406091 |
Aberrant ENPP2 expression promotes tumor progression in multiple myeloma [ Leuk Lymphoma, 2021, 1-12] | PubMed: 34847837 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。