PF-431396

製品コードS7644 バッチS764401

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

C22H21F3N6O3S
分子量 506.5 CAS No. 717906-29-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (197.43 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 5.000mg/ml (9.87mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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-431396 is a dual PYK2/FAK inhibitor with IC50 of 11 nM and 2 nM, respectively.
in vitro In A20 cells, PF-431396 blocks anti-Ig- and clustering LFA-1-induced tyrosine phosphorylation of Pyk2 and FAK, and further blocks B cell spreading. [2] This compound consistently inhibits the increase in protein tyrosine phosphorylation (PY) induced by the absence of added calcium and induced by W-7 in the presence of calcium. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Kinase assays and selectivity profiling
Kinase assays for PYK2 and FAK are determined as followed: unactivated full-length, C-terminal his-tagged human proteins are used in place of the Src-activated kinase domain protein and that test compounds are preincubated with enzyme for 1 h prior to the addition of 500 μM ATP. IC50 determinations are generated from 8 point dose response curves. Selectivity profiling against a diverse panel of kinases is performed by a commercial vendor and reported as average percent inhibition of duplicate tests.

参考

  • https://pubmed.ncbi.nlm.nih.gov/19244237/
  • https://pubmed.ncbi.nlm.nih.gov/19561089/
  • https://pubmed.ncbi.nlm.nih.gov/23595906/

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：

Vav2 is a master regulator of repair against bacterial pore-forming toxins [ bioRxiv, 2025, 2025.07.31.668026] PubMed: 40766405
The mechanism of L1 cell adhesion molecule interacting with protein tyrosine kinase 2 to regulate the focal adhesion kinase-growth factor receptor-bound protein 2-son of sevenless-rat sarcoma pathway in the identification and treatment of type I high-risk endometrial cancer [ Cytojournal, 2024, 21:34] PubMed: 39563667
Integrin signaling is critical for myeloid-mediated support of T-cell acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):6270] PubMed: 37805579
Integrin signaling is critical for myeloid-mediated support of T-cell acute lymphoblastic leukemia [ Nat Commun, 2023, 14(1):6270] PubMed: 37805579
Architecture of androgen receptor pathways amplifying glucagon-like peptide-1 insulinotropic action in male pancreatic β cells [ Cell Rep, 2023, 42(5):112529] PubMed: 37200193
Focal adhesion kinase inhibitor TAE226 combined with Sorafenib slows down hepatocellular carcinoma by multiple epigenetic effects [ J Exp Clin Cancer Res, 2021, 40(1):364] PubMed: 34784956
SHED-Dependent Oncogenic Signaling of the PEAK3 Pseudo-Kinase [ Cancers (Basel), 2021, 13(24)6344] PubMed: 34944965
A FAK/HDAC5 signaling axis controls osteocyte mechanotransduction [ Nat Commun, 2020, 11(1):3282] PubMed: 32612176
Myeloid cells provide critical support for T-ALL in vivo [ The University of Texas at Austin, 2020, ] PubMed: None
Inositol polyphosphate multikinase is a metformin target that regulates cell migration [ FASEB J, 2019, 33(12):14137-14146] PubMed: 31657647

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。