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Submit ReviewPQ 401 is an insulin-like growth factor receptor (IGF1R) inhibitor. Suppresses IGF-stimulated IGF-IR autophosphorylation with an IC50 value of 12 μM. Inhibits growth of MCF-7 breast cancer cells in vitro and in vivo.
PQ 401 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 341.79 |
公式 | C18H16ClN3O2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 196868-63-0 |
PubChem ID | 9549305 |
InChI Key | YBLWOZUPHDKFOT-UHFFFAOYSA-N |
Smiles | O=C(NC3=C(OC)C=CC(Cl)=C3)NC2=CC(C)=NC1=CC=CC=C12 |
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 | 17.09 | 50 | |
ethanol | 8.54 | 25 |
以下数据基于产品分子量 341.79。 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 | 5.85 mL | 29.26 mL | 58.52 mL |
2.5 mM | 1.17 mL | 5.85 mL | 11.7 mL |
5 mM | 0.59 mL | 2.93 mL | 5.85 mL |
25 mM | 0.12 mL | 0.59 mL | 1.17 mL |
参考文献是支持产品生物活性的出版物。
Anderson et al (2006) Parallel synthesis of diarylureas and their evaluation as inhibitors of Ins-like growth factor receptor. J.Comb.Chem. 8 784 PMID: 16961415
Sivakumar et al (2009) Autocrine loop for IGF-I receptor signaling in SLUG-mediated epithelial-mesenchymal transition. 34 329 PMID: 19148466
Gable et al (2006) Diarylureas are small-molecule inhibitors of Ins-like growth factor I receptor signaling and breast cancer cell growth. Mol.Cancer 5 1079 PMID: 16648580
If you know of a relevant reference for PQ 401, please let us know.
关键词: PQ 401, PQ 401 supplier, IGF-IR, inhibitors, inhibits, Receptors, Insulin-like, Receptor, Tyrosine, Kinases, RTKs, PQ401, Insulin, and, insulin-like, 2768, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 PQ 401 的部分引用包括:
Sanchez-Alavez et al (2011) Ins-like growth factor 1-mediated hyperthermia involves anterior hypothalamic Ins receptors. J Biol Chem 286 14983 PMID: 21330367
Jameson et al (2011) Activation of the Ins-like growth factor-1 receptor induces resistance to epidermal growth factor receptor antagonism in head and neck squamous carcinoma cells. Mol Cancer Ther 10 2124 PMID: 21878657
Ilatovskaya et al (2013) Pharmacological characterization of the P2 receptors profile in the podocytes of the freshly isolated rat glomeruli. Am J Physiol Cell Physiol 305 C1050 PMID: 24048730
Shen et al (2012) Ins-like growth factor (IGF) binding protein 2 functions coordinately with receptor protein tyrosine phosphatase β and the IGF-I receptor to regulate IGF-I-stimulated signaling. Mol Cell Biol 32 4116 PMID: 22869525
Radhakrishnan et al (2010) Ins-like growth factor-I-stimulated Ins receptor substrate-1 negatively regulates Src homology 2 domain-containing protein-tyrosine phosphatase substrate-1 function in vascular smooth muscle cells. J Biol Chem 285 15682 PMID: 20207740
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.