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)
Datasheet
Citations (1)
Literature
Pathways

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

BMS 536924 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 479.96
Formula C25H26ClN5O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 468740-43-4
PubChem ID 6077765
InChI Key DXEATJQGQHDURZ-DEDYPNTBSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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

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-κ27 3165 PMID: 17296734


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1 Citation for BMS 536924

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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Literature in this Area

Kinases

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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Peptides Involved in Appetite Modulation Scientific Review

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Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for BMS 536924

Insulin

Insulin Signaling Pathway

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

Protocols

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