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Submit ReviewPF 431396 is a dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively). Promotes osteoblast recruitment and activity, and stimulates bone formation in ovariectomized rats.
Sold for research purposes under agreement from Pfizer Inc.
PF 431396 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 506.5 |
公式 | C22H21F3N6O3S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 717906-29-1 |
PubChem ID | 11598628 |
InChI Key | POJZIZBONPAWIV-UHFFFAOYSA-N |
Smiles | O=C2NC1=CC=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC=C4N(C)S(=O)(C)=O)=N3)C=C1C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 25.32 | 50 |
以下数据基于产品分子量 506.5。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 3.95 mL | 19.74 mL | 39.49 mL |
2.5 mM | 0.79 mL | 3.95 mL | 7.9 mL |
5 mM | 0.39 mL | 1.97 mL | 3.95 mL |
25 mM | 0.08 mL | 0.39 mL | 0.79 mL |
参考文献是支持产品生物活性的出版物。
Buckbinder et al (2007) Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc.Natl.Acad.Sci.USA 104 10619 PMID: 17537919
Han et al (2009) Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. J.Biol.Chem. 284 13193 PMID: 19244237
Allen et al (2010) Emerging targets in osteoporosis disease modification. J.Med.Chem. 53 4332 PMID: 20218623
If you know of a relevant reference for PF 431396, please let us know.
关键词: PF 431396, PF 431396 supplier, PF431396, focal, adhesion, kinase, fak, proline-rich, tyrosine, 2, pyk2, inhibitors, inhibits, pfizer, Focal, Adhesion, Kinase, Other, Kinases, 4278, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PF 431396 的部分引用包括:
Santiago et al (2020) Cx43 and Associated Cell Signaling Pathways Regulate Tunneling Nanotubes in Breast Cancer Cells. Cancers (Basel) 12 PMID: 33003486
Kundumani-Sridharan et al (2013) 12/15-Lipoxygenase mediates high-fat diet-induced endothelial tight junction disruption and monocyte transmigration: a new role for 15(S)-hydroxyeicosatetraenoic acid in endothelial cell dysfunction. J Biol Chem 288 15830 PMID: 23589307
Pasquier et al (2018) CCL2/CCL5 secreted by the stroma induce IL-6/PYK2 dependent chemoresistance in ovarian cancer. Mol Cancer 17 47 PMID: 29455640
Cheng et al (2015) IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function. BMC Neurosci 212 513 PMID: 25779634
Chapman et al (2015) Proline-rich tyrosine kinase 2 controls PI3-kinase activation downstream of the T cell antigen receptor in human T cells. Sci Rep 97 285 PMID: 25387834
Brian et al (2019) Unique-region phosphorylation targets LynA for rapid degradation, tuning its expression and signaling in myeloid cells. Elife 8 PMID: 31282857
Kotla and Rao (2015) Reactive Oxygen Species (ROS) Mediate p300-dependent STAT1 Protein Interaction with Peroxisome Proliferator-activated Receptor (PPAR)-γ in CD36 Protein Expression and Foam Cell Formation. J Biol Chem 290 30306 PMID: 26504087
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
Winter et al (2012) Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML. Nat Chem Biol 8 905 PMID: 23023260
Mishra and Singh (2014) HIV-1 Tat C phosphorylates VE-cadherin complex and increases human brain microvascular endothelial cell permeability. J Leukoc Biol 15 80 PMID: 24965120
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