BMS 536924

Product Description

BMS 536924 is a 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.

Solubility

Preparing Stock Solutions for BMS 536924

The following data is based on the product molecular weight 479.96

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.08 mL	10.42 mL	20.84 mL
5 mM	0.42 mL	2.08 mL	4.17 mL
10 mM	0.21 mL	1.04 mL	2.08 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Kim Constitutively active type I Ins-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 Mol.Cell Biol. 2007 PMID: 17296734
• Huang The mechanisms of differential sensitivity to an Ins-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors. Cancer Res. 2009 PMID: 19117999
• Hendrickson Expression of Ins receptor isoform A and Ins-like growth factor-1 receptor in human acute myelogenous leukemia: effect of the dual-receptor inhibitor BMS-536924 in vitro. Cancer Res. 2009 PMID: 19789352
• Wittman Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of Ins-like growth factor I receptor kinase with in vivo antitumor activity. J.Med.Chem. 2005 PMID: 16134929