PQ 401

Short Summary : IGF1R inhibitor,potent and cell-permeable

Category : Tyrosine Kinase|IGF1R

Purity : 0.98

CAS Number : 196868-63-0

Formula : C18H16ClN3O2

Molecular Weight : 341.79

SMILE : CC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC

Solubility : >17.1mg/mL in DMSO

Storage : Store at -20°C

Description : PQ401 is a novel, potent inhibitor of IGF-IR with IC50 of 12M [1].In human MCF-7 cells, PQ401 inhibited autophosphorylation of the IGF-IR with IC50 of 12 M and autophosphorylation of the isolated kinase domain of the IGF-IR with IC50 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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