IGF-IR inhibitor, novel, potent and selective
CAS：475489-16-8
分子式：C27H29N5O
分子量：439.55
纯度：98%
存储：Store at -20°C

Background:

NVP-AEW541 is a novel, potent and selective inhibitor of IGF-IR kinase with IC50 value of 0.086 μM [1].

NVP-AEW541 is a pyrrolo(2,3-d) pyrimidine derivative. It has been reported to abolish IGF-I-induced IGF-IR autophosphorylation and to block the IGF-IR signaling pathway mainly in ECC-1 and USPC-1 cancer cells. Also in these cell lines, NVP-AEW541 has been shown to change the IGF-I induced cell cycle and to lead apoptotic cell death as well as exhibit antiproliferative effects [2]. In addition, it is observed that NVP-AEW541 can induce radiosensitization in PTEN wild-type cell lines [3].

Reference:
[1] Carlos Garc a-Echeverr a, Mark A.  Pearson, Andreas Marti, Thomas Meyer, Juergen Mestan, Johann Zimmermann, Jiaping Gao, Josef Brueggen, Hans-Georg Capraro, Robert Cozens, Dean B. Evans, Doriano Fabbro, Pascal Furet, Diana Graus Porta, Janis Liebetanz, Georg Martiny-Baron, Stephan Ruetz, and Francesco Hofmann. In vivo antitumor activity of NVP-AEW541—A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell.2004 Mar (5):231-239.
[2] Zohar Attias-Geva, Itay Bentov, Ami Fishman, Haim Werner, Ilan Bruchim.  Insulin-like growth factor-I receptor inhibition by speci c tyrosine kinase inhibitor NVP-AEW541 in endometrioid and serous papillary endometrial cancer cell lines. Gynecologic Oncology. 2011 Feb (121):383-389.
[3] Sofie F.  Isebaert, Johannes V. Swinnen, William H. Mcbride, and Karin M. Haustermans. Insulin-like growth factor–type 1 receptor inhibitor NVP-AEW541 enhances radiosensitivity of PTEN wild-type but not PTEN-deficient human prostate cancer cells. International Journal of Radiation Oncology Biology Physics. 2011 (81):239-247.