| Identification | Back Directory | [Name]
TYRPHOSTIN AG 1024 | [CAS]
65678-07-1 | [Synonyms]
AGS 200
Tyrphostin
AG-1024 (Tyrphostin)
2-(3-broMo-5-tert-butyl-4-hydroxybenzylidene)Malononitrile
2-[[3-Bromo-5-(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]propanedinitrile
2-[[3-Bromo-5-(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]propanedinitrile AGS 200 | [Molecular Formula]
C14H13BrN2O | [MDL Number]
MFCD02179365 | [MOL File]
65678-07-1.mol | [Molecular Weight]
305.174 |
| Hazard Information | Back Directory | [Description]
The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) initiates a cascade of reactions that promote cell growth and transformation by activating the PI3K/Akt signaling pathway, inhibiting apoptotic pathways, and mediating mitogenic actions. Overexpression of IGF-1R confers tumorigenic potential to cells as well as protection from apoptosis. AG-1024 is a selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC50 values of 0.4 and 7 μM, respectively. At 10 nM, AG-1024 can inhibit proliferation and induce apoptosis in human breast cancer MCF-7 cells, and it inhibits autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 μM. | [Uses]
Tyrphostin AG 1024 is an insulin-like growth factor (IGF)-I receptor antagonist. | [Definition]
ChEBI: 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile is an alkylbenzene. | [in vivo]
AG1024 (Tyrphostin AG 1024; 30 μg; i.p.; per day; for 2 weeks) significantly delays the tumour growth[1].
| Animal Model: | Female nude mice (6-8 weeks old)[1] | | Dosage: | 30 μg | | Administration: | IP; per day; for 2 weeks | | Result: | Significantly delayed the tumour growth.
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| [target]
IGF-1R | [References]
[1] párrizas m1, gazit a, levitzki a, wertheimer e, leroith d. specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. endocrinology. 1997 apr;138(4):1427-33.
[2] fan p1, agboke fa1, mcdaniel re1, sweeney ee1, zou x1, creswell k1, jordan vc2.inhibition of c-src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. eur j cancer. 2014 jan; 50(2):457-68. |
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Spectrum Chemical Manufacturing Corp.
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BOC Sciences
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NCE Biomedical Co.,Ltd.
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