Cat. No. 4774
Chemical Name: 4-[[(2S)-2-(3-Chlorophenyl)-2-hydro
Biological ActivityDual inhibitor of the insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) (IC50 values are 73 and 100 nM respectively). Inhibits receptor autophosphorylation and downstream MEK1/2 and Akt signaling. Induces G1 arrest and apoptosis in ML-1 cells; also inhibits cell proliferation in multiple tumor types. Reverses EMT through the attenuation of Snail mRNA expression in MCF10A cell over expressing IGF1R.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Hendrickson et al (2009) Expression of insulin receptor isoform A and insulin-like growth factor-1 receptor in human acute myelogenous leukemia: effect of the dual-receptor inhibitor BMS-536924 in vitro. Cancer Res. 69 7635. PMID: 19789352.
Huang et al (2009) The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors. Cancer Res. 69 161. PMID: 19117999.
Kim et al (2007) Constitutively active type I insulin-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is accompanied by an epithelial-to-mesenchymal transition mediated by NF-κB and snail. Mol.Cell Biol. 27 3165. PMID: 17296734.
Wittman et al (2005) Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J.Med.Chem. 48 5639. PMID: 16134929.
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Citations are publications that use Tocris products. Selected citations for BMS 536924 include:
Ising et al (2015) Inhibition of insulin/IGF-1 receptor signaling protects from mitochondria-mediated kidney failure. Front Behav Neurosci 7 275. PMID: 25643582.
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Keywords: BMS 536924, supplier, BMS536924, antitumor, antiproliferatives, insulin, receptor, IR, insulin-like, growth, factor-1, receptor, IGF1R, dual, inhibitors, inhibits, EMT, epithelial-to-mesenchymal, transition, Tocris Bioscience, Insulin and Insulin-like Receptors Inhibitor products
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