NVP-AEW541 is a reversible, ATP-competitive, orally available insulin-like growth factor-I receptor (IGF-IR, IGF-1R) inhibitor that, despite its equipotency against recombinant kinase domains of insulin receptor (InsR) and IGF-IR in cell-free kinase assays (IC50 = 140 & 150 nM, respectively), exhibits high selectivity toward cellular autophosphorylation of endogenous full-length IGF-1R (IC50 = 86 nM) over InsR (IC50 = 2.3 μM), HER1, PDGFR, c-Kit, and Bcr-Abl p210 (IC50 >5 μM). AEW541 effectively inhibits IGF-IR-mediated signaling and cancer survival (IC50 = 105 nM/MCF-7 soft agar growth, 1.64 μM/NWT-21 proliferation) in cultures and tumor growth in vivo (20 to 50 mg/kg twice daily p.o.; NWT-21 fibrosarcoma & TC-71 musculoskeletal sarcoma xenografts in mice).
Orally available insulin-like growth factor-I receptor inhibitor with in vitro and in vivo efficacy againsgt IGF-IR-mediated signaling and cancer survival.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Molecular cancer research : MCR, 10(6), 800-809 (2012-05-09)
NVP-AEW541, a specific ATP-competitive inhibitor of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase, has been reported to interfere with tumor growth in various tumor transplantation models. We have assessed the efficacy of NVP-AEW541 in repressing tumor growth and tumor
Identification of new drugs is strongly needed for sarcomas. Insulin-like growth factor-I receptor (IGF-IR) was found to provide a major contribution to the malignant behavior of these tumors, therefore representing a very promising therapeutic target. In this study, we analyzed
IGF-IR-mediated signaling promotes survival, anchorage-independent growth, and oncogenic transformation, as well as tumor growth and metastasis formation in vivo. NVP-AEW541 is a pyrrolo[2,3-d]pyrimidine derivative small molecular weight kinase inhibitor of the IGF-IR, capable of distinguishing between the IGF-IR (IC50 =
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