WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407199
CAS#: 196868-63-0
Description: PQ401 is a potent and selective IGF-1R inhibitor. PQ-401 induces apoptosis and inhibits growth, proliferation and migration of glioma cells. 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, administration of PQ401 on mice led to suppression of glioma tumour growth in vivo. PQ401 may serve as a promising leading drug for treating glioma patients with elevated IGF-1R signalling.
MedKoo Cat#: 407199
Name: PQ401
CAS#: 196868-63-0
Chemical Formula: C18H16ClN3O2
Exact Mass: 341.0931
Molecular Weight: 341.795
Elemental Analysis: C, 63.25; H, 4.72; Cl, 10.37; N, 12.29; O, 9.36
Synonym: PQ401; PQ-401; PQ 401.
IUPAC/Chemical Name: N-(5-Chloro-2-methoxyphenyl)-N'-(2-methyl-4-quinolinyl)urea
InChi Key: YBLWOZUPHDKFOT-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=CC(Cl)=CC=C3OC
1: Zhou X, Zhao X, Li X, Ping G, Pei S, Chen M, Wang Z, Zhou W, Jin B. PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells. J Chemother. 2015 May 14:1973947815Y0000000026. [Epub ahead of print] PubMed PMID: 25971682.
2: Ghosh MC, Gorantla V, Makena PS, Luellen C, Sinclair SE, Schwingshackl A, Waters CM. Insulin-like growth factor-I stimulates differentiation of ATII cells to ATI-like cells through activation of Wnt5a. Am J Physiol Lung Cell Mol Physiol. 2013 Aug 1;305(3):L222-8. doi: 10.1152/ajplung.00014.2013. Epub 2013 May 24. PubMed PMID: 23709620; PubMed Central PMCID: PMC3743013.
3: Jameson MJ, Beckler AD, Taniguchi LE, Allak A, Vanwagner LB, Lee NG, Thomsen WC, Hubbard MA, Thomas CY. 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. 2011 Nov;10(11):2124-34. doi: 10.1158/1535-7163.MCT-11-0294. Epub 2011 Aug 30. PubMed PMID: 21878657; PubMed Central PMCID: PMC3213311.
4: Troib A, Landau D, Youngren JF, Kachko L, Rabkin R, Segev Y. The effects of type 1 IGF receptor inhibition in a mouse model of diabetic kidney disease. Growth Horm IGF Res. 2011 Oct;21(5):285-91. doi: 10.1016/j.ghir.2011.07.007. Epub 2011 Aug 23. PubMed PMID: 21865067; PubMed Central PMCID: PMC4238882.
5: Sanchez-Alavez M, Osborn O, Tabarean IV, Holmberg KH, Eberwine J, Kahn CR, Bartfai T. Insulin-like growth factor 1-mediated hyperthermia involves anterior hypothalamic insulin receptors. J Biol Chem. 2011 Apr 29;286(17):14983-90. doi: 10.1074/jbc.M110.188540. Epub 2011 Feb 17. PubMed PMID: 21330367; PubMed Central PMCID: PMC3083203.
6: Lai VK, Linares-Palomino J, Nadal-Ginard B, Galiñanes M. Bone marrow cell-induced protection of the human myocardium: characterization and mechanism of action. J Thorac Cardiovasc Surg. 2009 Dec;138(6):1400-08.e1. doi: 10.1016/j.jtcvs.2009.07.013. Epub 2009 Aug 18. PubMed PMID: 19692000.
7: Sivakumar R, Koga H, Selvendiran K, Maeyama M, Ueno T, Sata M. Autocrine loop for IGF-I receptor signaling in SLUG-mediated epithelial-mesenchymal transition. Int J Oncol. 2009 Feb;34(2):329-38. PubMed PMID: 19148466.
8: Gable KL, Maddux BA, Penaranda C, Zavodovskaya M, Campbell MJ, Lobo M, Robinson L, Schow S, Kerner JA, Goldfine ID, Youngren JF. Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth. Mol Cancer Ther. 2006 Apr;5(4):1079-86. PubMed PMID: 16648580.