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BMS-536924

In stock
Catalog No.
A2238
IR/IGF-1R inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$180.00
In stock
5mg
$100.00
In stock
10mg
$170.00
In stock
50mg
$750.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

BMS-536924 is a novel inhibitor of IGF-1R with IC50 value of 100nM [1].

It has been found that BMS-536924 has cell toxicity in OVCAR-3 and OVCAR-4 cell lines. BMS-536924 inhibits cell proliferation partly via reducing phosphorylations of AKT and ribosomal protein S6, one of AKT’s downstream targets. [2].

BMS-536924 also induces apoptosis in vitro as indicated by the elevation of PARP-1 cleavage. It can induce DNA damage by the manner of increasing the phosphorylated histone H2AX as well as increasing the tail moment observed in the comet assay. It thus sensitizing cells to PARP inhibition [2].

References:
[1] Mark G. Saulnier, David B. Frennesson, Mark D. Wittman, Kurt Zimmermann, Upender Velaparthi, David R. Langley, Charles Struzynski, Xiaopeng Sang, Joan Carboni, Aixin Li, Ann Greer, Zheng Yang, Praveen Balimane, Marco Gottardis, Ricardo Attar and Dolatrai Vyas. 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924. Bioorganic & Medicinal Chemistry Letters. 2008 (18):1702-1707.
[2] Marie-Claude Beauchamp, Ariane Knafo, Amber Yasmeen, Joan M. Carboni, Marco M. Gottardis, Michael N. Pollak, Walter H. Gotlieb. BMS-536924 sensitizes human epithelial ovarian cancer cells to the PARP inhibitor, 3-aminobenzamide. Gynecologic Oncology. 2009 Aug (115):193-198.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt479.96
Cas No.468740-43-4
FormulaC25H26ClN5O3
Solubility≥24mg/mL in DMSO
Chemical Name(3E)-4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-(4-methyl-6-morpholin-4-yl-1,3-dihydrobenzimidazol-2-ylidene)pyridin-2-one
SDFDownload SDF
Canonical SMILESCC1=CC(=CC2=C1NC(=C3C(=CC=NC3=O)NCC(C4=CC(=CC=C4)Cl)O)N2)N5CCOCC5
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description BMS-536924 is a novel inhibitor of IGF-1R with IC50 value of 100 nM .
Targets IGF-1R          
IC50 100 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

BMS-536924