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Submit ReviewBMS 536924
说明： Dual IR/IGF1R inhibitor
化学名： 4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone
纯度： ≥98% (HPLC)
生物活性 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.
技术数据 for BMS 536924
| 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.
溶解性数据 for BMS 536924
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 48 | 100 |
制备储备液 for BMS 536924
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 |
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产品说明书 for BMS 536924
参考文献 for BMS 536924
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
9 篇 BMS 536924 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BMS 536924 的部分引用包括：
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
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
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