BMS 536924

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Cat.No. 4774 - BMS 536924 | C25H26ClN5O3 | CAS No. 468740-43-4
Description: Dual IR/IGF1R inhibitor
Chemical Name: 4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
Purity: ≥98% (HPLC)
Citations (4)

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.

Compound Libraries

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Technical Data

M. Wt 479.96
Formula C25H26ClN5O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 468740-43-4
PubChem ID 135440466
Smiles O=C1NC=CC(NC[C@H](C5=CC=CC(Cl)=C5)O)=C1C3=NC2=CC(N4CCOCC4)=CC(C)=C2N3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 48 100

Preparing Stock Solutions

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 will affect the solvent volumes required to prepare stock solutions.

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

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

Wittman et al (2005) 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. 48 5639 PMID: 16134929

Huang et al (2009) 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. 69 161 PMID: 19117999

Hendrickson et al (2009) 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. 69 7635 PMID: 19789352

Kim et al (2007) 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-κ27 3165 PMID: 17296734

If you know of a relevant reference for BMS 536924, please let us know.

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4 Citations for BMS 536924

Citations are publications that use Tocris products. Selected citations for BMS 536924 include:

Ising et al (2015) Inhibition of Ins/IGF-1 receptor signaling protects from mitochondria-mediated kidney failure. Front Behav Neurosci 7 275 PMID: 25643582

Augustin et al (2018) Impact of ins. signaling and proteasomal activity on physiological output of a neuronal circuit in aging Drosophila melanogaster. Neurobiol Aging 66 149 PMID: 29579685

Chinchore et al (2017) Glycolytic reliance promotes anabolism in photoreceptors. Elife 6 PMID: 28598329

Augustin et al (2017) Reduced ins. signaling maintains electrical transmission in a neural circuit in aging flies. PLoS Biol 15 e2001655 PMID: 28902870

Do you know of a great paper that uses BMS 536924 from Tocris? Please let us know.

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Literature in this Area

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
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Pathways for BMS 536924


Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.