NVP-AEW541

Short Summary : IGF-IR inhibitor, novel, potent and selective

Category : Tyrosine Kinase|IGF1R

Purity : 0.98

CAS Number : 475489-16-8

Formula : C27H29N5O

Molecular Weight : 439.55

SMILE : C1CN(C1)CC2CC(C2)N3C=C(C4=C3N=CN=C4N)C5=CC(=CC=C5)OCC6=CC=CC=C6

Solubility : >22mg/mL in DMSO

Storage : Store at -20°C

Description : NVP-AEW541 is a novel, potent and selective inhibitor of IGF-IR kinase with IC50 value of 0.086 M [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-AEW541A 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 factorCtype 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.

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