- BMS-754807
- GSK1904529A
- BMS-536924
- NVP-AEW541
- AG-1024
| PQ 401IGF1R inhibitor,potent and cell-permeable |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| 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 | |||||
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| Cas No. | 196868-63-0 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 1-(5-chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea | ||
| Canonical SMILES | CC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC | ||
| Formula | C18H16ClN3O2 | M.Wt | 341.79 |
| Solubility | ≥17.1mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | 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. | ||
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.
