PQ401 is a novel, potent inhibitor of IGF-IR with IC50 of 12μM .
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 . 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 .
In vivo, a treatment with PQ401 triple per week reduced the growth rate of MCNeuA cells implanted into mice .
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|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥17.1mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For 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.|
|Description||PQ 401 is a cell-permeable inhibitor of Insulin-like growth factor receptor (IGF1R) with IC50 value of 12 μM.|