BMS 536924

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Cat.No. 4774 - BMS 536924 | C25H26ClN5O3 | CAS No. 468740-43-4
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)
Datasheet
Citations (7)
Reviews
Literature (3)
Pathways (1)

Biological Activity

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.

Compound Libraries

BMS 536924 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48 100

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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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View Related Products by Product Action

View all Insulin and Insulin-like Receptor Inhibitors

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

7 Citations for BMS 536924

Citations are publications that use Tocris products. Selected citations for BMS 536924 include:

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

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.

Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for BMS 536924

Insulin

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.