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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. Find out more about compound libraries available from Tocris.
M. Wt | 341.79 |
Formula | C18H16ClN3O2 |
Storage | Store at +4°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 17.09 | 50 | |
ethanol | 8.54 | 25 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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.
Keywords: PQ 401, PQ 401 supplier, IGF-IR, inhibitors, inhibits, Receptors, Insulin-like, Receptor, Tyrosine, Kinases, RTKs, PQ401, Insulin, and, insulin-like, 2768, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for PQ 401 include:
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!
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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.