aew-541-cis-isomer

Description: NVP-AEW541 cis-isomer (also known as AEW541 cis-isomer), the cis-isomer of AEW541 is a novel and potent inhibitor of IGF-1R/InsR with IC50 of 150 nM/140 nM in cell-free assays, it has greater potency and selectivity for IGF-1R in a cell-based assay. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. In vivo, this orally bioavailable compound inhibits IGF-IR signaling in tumor xenografts and significantly reduces the growth of IGF-IR-driven fibrosarcomas. Thus, NVP- AEW541 represents a class of selective, small molecule IGF-IR kinase inhibitors with proven in vivo antitumor activity and potential therapeutic application.

References: Cancer Cell. 2004; 5(3):231-9; Cancer Res. 2005; 65(9):3868-76; Clin Cancer Res. 2006; 12(22):6772-80.

Related CAS: 475488-34-7 (free base); 475489-16-8 (cis-isomer free base); 1618643-96-1 (HCl); 2320261-63-8 (cis-isomer HCl)

Chemical Name: 7-((1r, 3r)-3-(azetidin-1-ylmethyl)cyclobutyl)-5-(3-(benzyloxy)phenyl)-7H-pyrrolo[2, 3-d]pyrimidin-4-amine

InChi Key: AECDBHGVIIRMOI-AQYVVDRMSA-N

InChi Code: InChI=1S/C27H29N5O/c28-26-25-24(21-8-4-9-23(14-21)33-17-19-6-2-1-3-7-19)16-32(27(25)30-18-29-26)22-12-20(13-22)15-31-10-5-11-31/h1-4, 6-9, 14, 16, 18, 20, 22H, 5, 10-13, 15, 17H2, (H2, 28, 29, 30)/t20-, 22-

SMILES Code: NC1=C2C(N([CH]3C[CH](CN4CCC4)C3)C=C2C5=CC=CC(OCC6=CC=CC=C6)=C5)=NC=N1