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Tocris/BMS 536924/4774/50/50 mg

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货号: 4774/50

品牌: Tocris

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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 Technical Data Solubility Calculators Datasheets References

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 Plus. 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	6077765
InChI Key	DXEATJQGQHDURZ-DEDYPNTBSA-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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 solvent 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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Wittman et al (2005) Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-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 insulin-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 insulin receptor isoform A and insulin-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 insulin-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-κ27 3165 PMID: 17296734

Keywords: BMS 536924, supplier, BMS536924, antitumor, antiproliferatives, insulin, receptor, IR, insulin-like, growth, factor-1, receptor, IGF1R, dual, inhibitors, inhibits, EMT, epithelial-to-mesenchymal, transition, Insulin, and, insulin-like, Receptors, Insulin, and, Insulin-like, Receptors, Insulin, and, insulin-like, Receptors, Tocris Bioscience

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