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Submit ReviewBMS 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.
分子量 | 479.96 |
公式 | C25H26ClN5O3 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 48 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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-κ
Mol.Cell Biol. 27
3165 PMID: 17296734
If you know of a relevant reference for BMS 536924, please let us know.
关键词: BMS 536924, BMS 536924 supplier, BMS536924, antitumor, antiproliferatives, insulin, receptor, IR, insulin-like, growth, factor-1, IGF1R, dual, inhibitors, inhibits, EMT, epithelial-to-mesenchymal, transition, Insulin, and, Receptors, Insulin-like, 4774, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BMS 536924 的部分引用包括:
Bradley J et al (2022) Epiregulin as an Alternative Ligand for Leptin Receptor Alleviates Glucose Intolerance without Change in Obesity. Cells 11 PMID: 35159237
David C et al (2020) mTORC2 Assembly Is Regulated by USP9X-Mediated Deubiquitination of RICTOR. Cell Rep 33 108564 PMID: 33378666
Augustin et al (2017) Reduced ins. signaling maintains electrical transmission in a neural circuit in aging flies. PLoS Biol 15 e2001655 PMID: 28902870
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
Ising et al (2015) Inhibition of Ins/IGF-1 receptor signaling protects from mitochondria-mediated kidney failure. Front Behav Neurosci 7 275 PMID: 25643582
Uchikawa et al (2019) Activation mechanism of the Ins. receptor revealed by cryo-EM structure of the fully liganded receptor-ligand complex. Elife 8 PMID: 31436533
Demian et al (2019) The Ion Transporter NKCC1 Links Cell Volume to Cell Mass Regulation by Suppressing mTORC1. Cell Rep 27 1886 PMID: 31067471
Choi et al (2019) Mitotic regulators and the SHP2-MAPK pathway promote IR endocytosis and feedback regulation of Ins. signaling. Nat Commun 10 1473 PMID: 30931927
Chinchore et al (2017) Glycolytic reliance promotes anabolism in photoreceptors. Elife 6 PMID: 28598329
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.