P0113
PQ401
≥98% (HPLC), powder
Synonym(s):
IGF-1R Inhibitor II, N-(5-Chloro-2-methoxyphenyl)-N′-(2-methylquinolin-4-yl)urea
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About This Item
Empirical Formula (Hill Notation):
C18H16ClN3O2
CAS Number:
Molecular Weight:
341.79
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white
solubility
DMSO: >10 mg/mL
H2O: <2 mg/mL
storage temp.
2-8°C
SMILES string
COc1ccc(Cl)cc1NC(=O)Nc2cc(C)nc3ccccc23
InChI
1S/C18H16ClN3O2/c1-11-9-15(13-5-3-4-6-14(13)20-11)21-18(23)22-16-10-12(19)7-8-17(16)24-2/h3-10H,1-2H3,(H2,20,21,22,23)
InChI key
YBLWOZUPHDKFOT-UHFFFAOYSA-N
Application
PQ401 has been used as:
- an insulin growth factor-1 receptor (IGF-IR) inhibitor in H1299 cells to test its effect on migration suppression
- a reference inhibitor in dose-response measurements studies
- an IGF1R inhibitor in sirtuin 6 (SIRT6)-deficient cardiomyocytes to test its effect on hypertrophy inhibition
Biochem/physiol Actions
PQ401 is an insulin growth factor-1 receptor (IGF-1R) inhibitor.
PQ401, a diaryl urea compound that serves as an anti-glioma agent.
Features and Benefits
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the InsR page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Personal Protective Equipment
dust mask type N95 (US), Eyeshields, Gloves
Regulatory Information
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Monica Brenca et al.
The Journal of pathology, 238(4), 543-549 (2015-11-27)
Gastrointestinal stromal tumours (GISTs) are the most common mesenchymal neoplasms of the gastrointestinal tract. The vast majority of GISTs are driven by oncogenic activation of KIT, PDGFRA or, less commonly, BRAF. Loss of succinate dehydrogenase complex activity has been identified
Xiang Zhou et al.
Journal of chemotherapy (Florence, Italy), 28(1), 44-49 (2015-05-15)
Growth factor signalling pathways transduce extra-cellular physiological cues to guide cells to maintain critical cellular functions, including cell proliferation, survival and metabolism. Dysregulation of certain growth factor signalling pathways has been shown as a major route to promote tumourigenesis. Glioma
Gang Xi et al.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 29(11), 2427-2438 (2014-05-20)
Insulin-like growth factor binding protein 2 (IGFBP-2) is important for acquisition of normal bone mass in mice; however, the mechanism by which IGFBP-2 functions is not defined. These studies investigated the role of IGFBP-2 in stimulating osteoblast differentiation. MC-3T3 preosteoblasts
Jung-Min Choi et al.
Lung cancer (Amsterdam, Netherlands), 90(2), 175-181 (2015-09-08)
Lung cancer is the commonly diagnosed cancer and is the leading cause of cancer-related mortality worldwide. The most prevalent form of lung cancer is NSCLC, comprising 80% of all lung cancer cases, and epidermal growth factor receptor (EGFR) is frequently
Identification of Novel IGF1R Kinase Inhibitors by Molecular Modeling and High-Throughput Screening.
R Moriev et al.
Acta naturae, 5(2), 90-99 (2013-07-03)
The aim of this study was to identify small molecule compounds that inhibit the kinase activity of the IGF1 receptor and represent novel chemical scaffolds, which can be potentially exploited to develop drug candidates that are superior to the existing
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