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Submit ReviewBMS 536924
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)
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 Data for BMS 536924
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| 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 |
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Product Datasheets for BMS 536924
References for BMS 536924
References are publications that support the biological activity of the product.
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.
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Keywords: 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 Citations for BMS 536924
Citations are publications that use Tocris products. Selected citations for BMS 536924 include:
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
Augustin et al (2017) Reduced ins. signaling maintains electrical transmission in a neural circuit in aging flies. PLoS Biol 15 e2001655 PMID: 28902870
Do you know of a great paper that uses BMS 536924 from Tocris? Please let us know.
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Pathways for BMS 536924
