For research use only, not for therapeutic use.
PQ401 (Cat No.:I002508) is a selective inhibitor of insulin-like growth factor-1 receptor (IGF1R) autophosphorylation, with an IC50 of <1 μM. It demonstrates activity against cultured human MCF-7 breast cancer cells, inhibiting IGF1R autophosphorylation and growth with IC50 values of 12 μM and 6 μM, respectively. PQ401 induces caspase-mediated apoptosis and shows potential in regulating thermoregulation. In vivo studies suggest its impact on normal kidneys, causing renal hypertrophy and collagen/fat accumulation. However, it does not significantly affect the parameters of diabetic kidney disease.
| Catalog Number | I002508 |
| CAS Number | 196868-63-0 |
| Synonyms | 1-(5-chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea |
| Molecular Formula | C18H16ClN3O2 |
| Purity | ≥95% |
| Target | IGF1R |
| Solubility | 50 mM in DMSO and to 25 mM in ethanol |
| Storage | 3 years -20C powder |
| IC50 | 12 uM (inhibited autophosphorylation of the IGF-IR in cultured human MCF-7 cells) |
| IUPAC Name | 1-(5-chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea |
| InChI | 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) |
| InChIKey | YBLWOZUPHDKFOT-UHFFFAOYSA-N |
| SMILES | CC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC |
| Reference | 1:J Chemother. 2016;28(1):44-9. doi: 10.1179/1973947815Y.0000000026. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells.Zhou X,Zhao X,Li X,Ping G,Pei S,Chen M,Wang Z,Zhou W,Jin B, PMID: 25971682 DOI: 10.1179/1973947815Y.0000000026 </br><span>Abstract:</span> 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 is a type of aggressive malignant tumour with no effective systematic therapy so far. Overexpression or hyperactivation of IGF-1R has been observed to be tightly associated with glioma progression and poor prognosis. Here, we examined the biological effects of a specific IGF-1R inhibitor, PQ401, on suppressing U87MG glioma cell growth and migration. Specifically, we observed that PQ401 not only induced cellular apoptosis in U87MG cells and subsequently reduced cell viability and proliferation but also attenuated cell mobility in vitro. More importantly, through a mouse xenograft model, we observed that administration of PQ401 on mice led to suppression of glioma tumour growth in vivo. In summary, our study suggests that PQ401 may serve as a promising leading drug for treating glioma patients with elevated IGF-1R signalling. |
