Catalog Number: 4774
Chemical Name: 4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
Biological Activity
Dual 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.
Technical Data
  • M.Wt:
    479.96
  • Formula:
    C25H26ClN5O3
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    468740-43-4
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.
Background References
  1. 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.
    Wittman et al.
    J.Med.Chem., 2005;48:5639
  2. The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors.
    Huang et al.
    Cancer Res., 2009;69:161
  3. 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.
    Hendrickson et al.
    Cancer Res., 2009;69:7635
  4. 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-κ
    Kim et al.
    Mol.Cell Biol., 2007;27:3165
Citations:

The citations listed below are publications that use Tocris products. Selected citations for BMS 536924 include:

1 Citations: Showing 1 - 1

  1. Inhibition of insulin/IGF-1 receptor signaling protects from mitochondria-mediated kidney failure.
    Authors: Ising Et al.
    Front Behav Neurosci 2015;7:275

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