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BMS-536924
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-536924图片
CAS NO:468740-43-4
规格:98%
分子量:479.96
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
IR/IGF-1R inhibitor
CAS:468740-43-4
分子式:C25H26ClN5O3
分子量:479.96
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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.