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化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C22H20F3N5O3S |
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| 分子量 | 491.49 | CAS No. | 869288-64-2 | |
| Solubility (25°C)* | 体外 | DMSO | 26 mg/mL (52.9 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM in a cell-free assay, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. PF-573228 induces apoptosis. |
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| in vitro | PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover. [1] |
| in vivo | Inhibition of FAK by PF-573,228 in Ctrl-MT mice leads to a significant suppression of mammary tumorigenesis as well as lung metastasis. In contrast, treatment of MFCKO-MT mice with PF-573,228 did not affect the initiation of mammary tumors in these mice, as would be expected due to the absence of FAK in mammary epithelial cells of these mice [2]. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Affinity determination | |
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| Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3 | ||
| 細胞アッセイ | 細胞株 | REF52 or PC3 cells |
| 濃度 | ~10 μM | |
| 反応時間 | 3 days | |
| 実験の流れ | Growth assays are performed by seeding 1 × 104 REF52 or PC3 cells/well of a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor for 3 days. Subsequently, the cells are harvested and counted. |
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| 動物実験 | 動物モデル | Ctrl-MT and MFCKO-MT mice |
| 投薬量 | 5 mg/kg | |
| 投与方法 | oral administration | |
参考
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カスタマーフィードバック
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Data from [PLoS One, 2014, 9(2), e88588]
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, 2014, Dr.Milica Pesic from Institute for Biological Research
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, , Nature, 2016, 537(7620):422-429.
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：
| Non-catalytic role of phosphoinositide 3-kinase in mesenchymal cell migration through non-canonical induction of p85β/AP2-mediated endocytosis [ Nat Commun, 2024, 15(1):2612] | PubMed: 38521786 |
| Cancer-associated fibroblast-derived periostin promotes papillary thyroid tumor growth through integrin-FAK-STAT3 signaling [ Theranostics, 2024, 14(7):3014-3028] | PubMed: 38773979 |
| Sustained intestinal epithelial monolayer wound closure after transient application of a FAK-activating small molecule [ PLoS One, 2024, 19(8):e0304010] | PubMed: 39150901 |
| Tenascin-C in the early lung cancer tumor microenvironment promotes progression through integrin αvβ1 and FAK [ bioRxiv, 2024, 2024.09.17.613509] | PubMed: 39345541 |
| Carboxymethyl chitosan-alginate enhances bone repair effects of magnesium phosphate bone cement by activating the FAK-Wnt pathway [ Bioact Mater, 2023, 20:598-609] | PubMed: 35846837 |
| Mutant p53 sustains serine-glycine synthesis and essential amino acids intake promoting breast cancer growth [ Nat Commun, 2023, 14(1):6777] | PubMed: 37880212 |
| The Tumor Suppressor DAB2IP Is Regulated by Cell Contact and Contributes to YAP/TAZ Inhibition in Confluent Cells [ Cancers (Basel), 2023, 15(13)3379] | PubMed: 37444489 |
| The Tumor Suppressor DAB2IP Is Regulated by Cell Contact and Contributes to YAP/TAZ Inhibition in Confluent Cells [ Cancers (Basel), 2023, 15(13)3379] | PubMed: 37444489 |
| Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adh Migr, 2023, 17(1):1-14] | PubMed: 36944577 |
| Inhibition of Integrin αvβ3-FAK-MAPK signaling constrains the invasion of T-ALL cells [ Cell Adhesion & Migration, 2023, 17(1)] | PubMed: None |
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。