PQ 401

立即咨询

PQ 401

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

196868-63-0

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
25mg	电议
100mg	电议

产品介绍

PQ 401 是一种有效的 IGF-IR 信号抑制剂。在 MCF-7 细胞的一系列研究中，PQ 401 抑制 IGF-I 刺激的 IGF-IR 自磷酸化，IC5\u200b\u200b0 为 12.0 μM。 PQ 401 可有效抑制 IGF-I 刺激的 MCF-7 细胞生长 (IC50, 6 μM)。 PQ 401 是治疗乳腺癌和其他 IGF-I 敏感癌症的潜在药物。 PQ 401 诱导半胱天冬酶介导的细胞凋亡。

Cas No.	196868-63-0
化学名	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
分子式	C₁₈H₁₆ClN₃O₂
分子量	341.79
溶解度	≥ 17.1mg/mL in DMSO
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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.