PQ 401 |
Catalog No.GC16991 |
PQ 401은 IGF-IR 신호전달의 강력한 억제제입니다. PQ 401은 MCF-7 세포에 대한 일련의 연구에서 12.0μM의 IC50으로 IGF-I 자극 IGF-IR 자가인산화를 억제합니다. PQ 401은 MCF-7 세포(IC50, 6μM)의 IGF-I 자극 성장 억제에 효과적입니다. PQ 401은 유방암 및 기타 IGF-I에 민감한 암의 잠재적인 약제입니다. PQ 401은 카스파제 매개 세포자멸사를 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 196868-63-0
Sample solution is provided at 25 µL, 10mM.
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.
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