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Protein Tyrosine Kinase
IGF-1R
IGF-1R
下级目录
GSK-1904529a
Insulin-likeGrowthFactor-1ReceptorInhibitor
TYRPHOSTIN AG 1024
Linsitinib
(2S)-1-[4-[(5-Cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridyl)-2-methyl-pyrrolidine-2-carboxamide
目录项下的产品
1089283-49-7 / MFCD189283497
GSK-1904529A, also known as GSK 4529, is an IGF-1R Inhibitor, is is a promising candidate for therapeutic use in IGF-IR–dependent tumors. GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. GSK1904529A blocks receptor autophosphorylation and downstream signaling, leading to cell cycle arrest. It inhibits the proliferation of cell lines derived from solid and hematologic malignancies, with multiple myeloma and Ewing's sarcoma cell lines being most sensitive. Oral administration of GSK1904529A decreases the growth of human tumor xenografts in mice, consistent with a reduction of IGF-IR phosphorylation in tumors. Despite the potent inhibitory activity of GSK1904529A on IR in vitro and in vivo , minimal effects on blood glucose levels are observed in animals at doses that show significant antitumor activity. (source: Clin Cancer Res May 1, 2009 15; 3058 )
GSK1904529A游离态
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468740-43-4 / MFCD68740434
(S)-4-((2-(3-Chlorophenyl)-2-hydroxyethyl)amino)-3-(4-methyl-6-morpholino-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one
(S)-4-((2-(3-氯苯基)-2-羟乙基)氨基)-3-(4-甲基-6-吗啉-1H-苯并[d]咪唑-2-基)吡啶-2(1H)-酮
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中华人民共和国
65678-07-1 / MFCD02179365
AG-1024 is also called Tyrphostin, is a selective inhibitor of IGF-1R. AG-1024 was used to evaluate effects on proliferation, radiosensitivity, and radiation-induced cell apoptosis in a human breast cancer cell line MCF-7. Exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in a time-dependent manner, and the degree of growth inhibition for IC20 plus irradiation (4 Gy) was up to 50% compared to the control. Tyrphostin AG 1024 could be used as a potential therapeutic agent in combination with irradiation.
2-(3-溴-5-(叔丁基)-4-羟基亚苄基)丙二腈
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867160-71-2 / MFCD12912153
Cis-3-(8-Amino-1-(2-Phenylquinolin-7-Yl)Imidazo[1,5-A]Pyrazin-3-Yl)-1-Methylcyclobutan-1-Ol
顺式-3-(8-氨基-1-(2-苯基喹啉-7-基)咪唑并[1,5-a]吡嗪-3-基)-1-甲基环丁醇
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1001350-96-4 / MFCD18633202
(S)-1-(4-((5-Cyclopropyl-1H-Pyrazol-3-Yl)Amino)Pyrrolo[2,1-F][1,2,4]Triazin-2-Yl)-N-(6-Fluoropyridin-3-Yl)-2-Methylpyrrolidine-2-Carboxamide
(S)-1-(4-((5-环丙基-1H-吡唑-3-基)氨基)吡咯[2,1-f][1,2,4]三嗪-2-基)-N-(6-氟吡啶-3-基)-2-甲基吡咯烷-2-甲酰胺
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