| Hazard Information | Back Directory | [Description]
AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder scholar made mistake - AEW541 was mistakenly listed as CAS#475488-34-7, the trans-isomer of AEW541. The correct structure of AEW541 can be confirmed from Joel Slade, et al (from Novartis), Org. Process Res. Dev. 2007, 11, 5, 825–835. | [Uses]
NVP-AEW541 dihydrochloride (AEW541 dihydrochloride) is an orally active inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with an IC50 value of 0.15 μM. NVP-AEW541 dihydrochloride also inhibits InsR, IC50 with a value of 0.14 μM. NVP-AEW541 dihydrochloride has antitumor activity[1]. | [References]
[1] García-Echeverría C, et al. In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell. 2004 Mar;5(3):231-9. DOI:10.1016/s1535-6108(04)00051-0 |
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