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PQ 401

In stock
Catalog No.
A2033
IGF1R inhibitor,potent and cell-permeable
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$106.00
In stock
5mg
$50.00
In stock
25mg
$200.00
In stock
100mg
$630.00
In stock

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Background

PQ401 is a novel, potent inhibitor of IGF-IR with IC50 of 12μM [1].

In human MCF-7 cells, PQ401 inhibited autophosphorylation of the IGF-IR with IC50 of 12 μM and autophosphorylation of the isolated kinase domain of the IGF-IR with IC50 < 1μM. In addition, PQ401 inhibited the growth of cultured breast cancer cells in serum at 10μM. PQ401 can decrease IGF-I-mediated signaling through the Akt antiapoptotic pathway. Twenty-four hours treatment of 15 μM PQ401 induced caspase-mediated apoptosis [1]. In small trigeminal ganglion neurons, PQ401 blocked the IGF-1-induced A-type K(+) currents (IA) that were associated with a hyperpolarizing shift in the voltage dependence of inactivation [2].

In vivo, a treatment with PQ401 triple per week reduced the growth rate of MCNeuA cells implanted into mice [1].

References:
[1]. 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.
[2]. Wang H, Qin J, Gong S, Feng B, Zhang Y, Tao J. Insulin-like growth factor-1 receptor-mediated inhibition of A-type K(+) current induces sensory neuronal hyperexcitability through the phosphatidylinositol 3-kinase and extracellular signal-regulated kinase 1/2 pathways, independently of Akt. Endocrinology. 2014 Jan;155(1):168-79.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt341.79
Cas No.196868-63-0
FormulaC18H16ClN3O2
Solubility≥17.1mg/mL in DMSO
Chemical Name1-(5-chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea
SDFDownload SDF
Canonical SMILESCC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description PQ 401 is a cell-permeable inhibitor of Insulin-like growth factor receptor (IGF1R) with IC50 value of 12 μM.
Targets IGF1R          
IC50 12 μM          

Quality Control

Quality Control & MSDS

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Chemical structure

PQ 401