Chemical Name : GSK1904529A
CAS : 1089283-49-7
Solubility:Soluble in DMSO at 10 mmol/L
Storage:-20C 2 years
GSK1904529A, which potently inhibits IGF-IR and IR activities in vitro and in vivo, is a promising candidate for therapeutic use in solid and hematologic cancers.GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively.IC50s for GSK1904529A in tumor cell lines ranged from 35 nmol/L to >30 umol/L. The tumor histologic types showing the greatest sensitivity to this compound were Ewing's sarcoma and multiple myeloma, where IC50s in three of five Ewing's sarcoma cell lines were <100 nmol/L and IC50s in five of eight multiple myeloma cell lines were <200 nmol/L.Oral administration of GSK1904529A decreases the growth of human tumor xenografts in mice.
1. Sabbatini P, Rowand JL, Groy A, Korenchuk S, Liu Q, Atkins C, Dumble M, Yang J, Anderson K, Wilson BJ, Emmitte KA, Rabindran SK, Kumar R. Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase. Clin Cancer Res. 2009 May 1;15(9):3058-67. Epub 2009 Apr 21