PF-8380

製品コードS8218 バッチS821804

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H21Cl2N3O5
分子量 478.33 CAS No. 1144035-53-9
Solubility (25°C)* 体外 DMSO 96 mg/mL (200.69 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 PF-8380 is a potent autotaxin inhibitor with IC50 of 2.8nM in an in vitro enzyme assay.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mouse GL261 and Human U87-MG cells
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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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