AG-1024

The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) initiates a cascade of reactions that promote cell growth and transformation by activating the PI3K/Akt signaling pathway, inhibiting apoptotic pathways, and mediating mitogenic actions. Overexpression of IGF-1R confers tumorigenic potential to cells as well as protection from apoptosis. AG-1024 is a selective inhibitor of IGF-1R that inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation with IC50 values of 0.4 and 7 µM, respectively. At 10 nM, AG-1024 can inhibit proliferation and induce apoptosis in human breast cancer MCF-7 cells, and it inhibits autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 µM.Formal Name: 2-[[3-bromo-5-(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-propanedinitrile. CAS Number: 65678-07-1. Synonyms: AGS 200, Tyrphostin AG-1024. Molecular Formula: C14H13BrN2O. Formula Weight: 305.2. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 16 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 1.6 mg/ml. lambdamax: 255, 348, 359, 452 nm. SMILES: BrC1=C(O)C(C(C)(C)C)=CC(/C=C(C#N)/C#N)=C1. InChi Code: InChI=1S/C14H13BrN2O/c1-14(2,3)11-5-9(4-10(7-16)8-17)6-12(15)13(11)18/h4-6,18H,1-3H3. InChi Key: ABBADGFSRBWENF-UHFFFAOYSA-N.