PQ 401

Pricing Availability Delivery Time Qty
Cat.No. 2768 - PQ 401 | C18H16ClN3O2 | CAS No. 196868-63-0
Description: IGF1R inhibitor
Chemical Name: N-(5-Chloro-2-methoxyphenyl)-N'-(2-methyl-4-quinolinyl)urea
Purity: ≥99% (HPLC)
Datasheet
Citations (5)
Literature
Pathways

Biological Activity

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.

Compound Libraries

PQ 401 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 17.09 50
ethanol 8.54 25

Preparing Stock Solutions

The following data is based on the product molecular weight 341.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.93 mL 14.63 mL 29.26 mL
5 mM 0.59 mL 2.93 mL 5.85 mL
10 mM 0.29 mL 1.46 mL 2.93 mL
50 mM 0.06 mL 0.29 mL 0.59 mL

Molarity Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Anderson et al (2006) Parallel synthesis of diarylureas and their evaluation as inhibitors of insulin-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 insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol.Cancer 5 1079 PMID:


If you know of a relevant reference for PQ 401, please let us know.

View Related Products by Product Action

View all Insulin and Insulin-like Receptor Inhibitors

Keywords: IGF-IR inhibitors inhibits Receptors Insulin-like Receptor Tyrosine Kinases RTKs PQ401 Insulin and insulin-like Receptors

5 Citations for PQ 401

Citations are publications that use Tocris products. Selected citations for PQ 401 include:

Sanchez-Alavez et al (2011) Insulin-like growth factor 1-mediated hyperthermia involves anterior hypothalamic insulin receptors. J Biol Chem 286 14983 PMID: 21330367

Jameson et al (2011) Activation of the insulin-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

Radhakrishnan et al (2010) Insulin-like growth factor-I-stimulated insulin 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

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) Insulin-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


Do you know of a great paper that uses PQ 401 from Tocris? If so please let us know.

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Reviews

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Literature in this Area

Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

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.

Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for PQ 401

Insulin

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.

Protocols

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