BMS 536924

Name: BMS 536924
Brand: Tocris Bioscience
SKU: 4774

Tocris Bioscience, part of Bio-Techne | Catalog # 4774

Citations (22)

COA / SDS

Dual IR/IGF1R inhibitor

Key Product Details

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)
Molecular Weight:	479.96

View Full Technical Details for BMS 536924

Technical Data
Citations

Biological Activity for BMS 536924

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.

Technical Data for BMS 536924

M. Wt	479.96
Formula	C₂₅H₂₆ClN₅O₃
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	468740-43-4
PubChem ID	135440466
InChi Key	ZWVZORIKUNOTCS-OAQYLSRUSA-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.

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

Solubility for BMS 536924

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

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 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for BMS 536924

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