GSK1904529A

GSK1904529A

GSK1904529A

编号ABP000158 化学名称GSK1904529A CAS1089283-49-7 分子式C44H47F2N9O5S 分子量851.963 纯度 >99%

化学名称 : GSK1904529A

CAS : 1089283-49-7

英文名称: GSK1904529A

英文同义词: N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide

溶解度:Soluble in DMSO at 10 mmol/L

储存条件:-20C 2 years

生物活性

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.

参考文献

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

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