A dual inhibitor of IGF-1R kinase and IR (IC50s = 100 and 73 nM

BMS-536924 – 5 mg

Brand:
Cayman
CAS:
468740-43-4
Storage:
-20
UN-No:
Non-Hazardous - /

BMS-536924 is a dual inhibitor of insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IC50s = 100 and 73 nM, respectively).{29658} In this way, it blocks IGF-1R autophosphorylation and signaling through MEK1/2 and Akt, leading to G1 arrest and apoptosis in myeloblastic leukemia ML-1 cells. BMS-536924 reverses epithelial-to-mesenchymal transition in immortalized mammary epithelial MCF10A cells overexpressing constitutively activated IGF-1R and causes growth inhibition and polarization of breast cancer MCF-7 cells.{29655,29657} It also induces expression of cytochrome P450 3A4 isoform in primary hepatocytes.{29656}  

 

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Description

A dual inhibitor of IGF-1R kinase and IR (IC50s = 100 and 73 nM, respectively); blocks IFG-1R autophosphorylation and signaling through MEK1/2 and Akt, leading to G1 arrest and apoptosis in ML-1 cells; reverses EMT in MCF10A cells overexpressing constitutively activated IGF-1R

Formal name: 4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone

Synonyms: 

Molecular weight: 480

CAS: 468740-43-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|IGF-1R/InsR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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