Cat. No. Name Size Price Add Cart
KI1334NVP-AEW5412 mg$336
NVP-AEW5415 mg$592
NVP-AEW54110 mg$1072
NVP-AEW54150 mg$3152

Chemical Characteristic

Product NameNVP-AEW541
CAS No.475489-16-8
Molecular Weight 439.55
FormulaC27H29N5O
Chemical Name7-((1s,3s)-3-(azetidin-1-ylmethyl)cyclobutyl)-5-(3-(benzyloxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
SmilesNc1c2c(ncn1)n(cc2c1cc(ccc1)OCc1ccccc1)C1C[C@H](C1)CN1CCC1
Chemical Structure

Biological activities

NVP-AEW541 is a novel, potent, and selective inhibitor of the IGF-IR kinase. The IC50 of NVP-AEW541 is 86 nM against IGF-IR. NVP-AEW541 inhibits the closely related InsR (insulin receptor) with an IC50 of 2.3 µM. NVP-AEW541 abrogates IGF-I-mediated survival, as well as colony formation, in soft agar at concentrations which are in agreement with inhibition of IGF-IR autophosphorylation. NVP-AEW541 prevents HER-1, HER-2, and HER-4 with IC50 of 5.8, 4.1 and 1.4 µM, respectively.[1] It is also reported that NVP-AEW541 inhibits IGF-I-mediated receptor activation and downstream signaling.[2] NVP-AEW541 reduces the activation of IGF-IR, IRS-1, Erk, Akt and STAT3. Furthermore, NVP-AEW541 decreases cancer cell proliferation and abrogates migratory effects of IGF-I. NVP-AEW541 directly affects on endothelial cells in terms of reducing endothelial cell migration.[3] NVP-AEW541 treatment (24 hours) induces dephosphorylation of IGF-IR. NVP-AEW541 also gives rise to Akt dephosphorylation and changes in the expression of key regulatory proteins of the cell cycle.[4] In vivo, NVP-AEW541 inhibits IGF-IR signaling in tumor xenografts and significantly reduces the growth of IGF-IR-driven fibrosarcomas.[1] Combined treatment with NVP-AEW541 and vincristine significantly prevents tumor growth of Ewing's sarcoma xenografts in nude mice.[2] NVP-AEW541 significantly downregulates orthotopic pancreatic tumour growth, vascularisation, and VEGF expression.[3]

Protocols

In vitro: NVP-AEW541 is prepared in DMSO and stored at -20 °C. [2]

References

[1] Garc?a-Echeverr?a 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):231-239.
[2] Scotlandi K, et al. Antitumor activity of the insulin-like growth factor-I receptor kinase inhibitor NVP-AEW541 in musculoskeletal tumors. Cancer Res. 2005, 65(9): 3868-3876.
[3] Moser C, et al. Inhibition of insulin-like growth factor-I receptor (IGF-IR) using NVP-AEW541, a small molecule kinase inhibitor, reduces orthotopic pancreatic cancer growth and angiogenesis. Eur J Cancer. 2008, 44(11): 1577-1586.
[4] Tazzari PL, et al. The insulin-like growth factor-I receptor kinase inhibitor NVP-AEW541 induces apoptosis in acute myeloid leukemia cells exhibiting autocrine insulin-like growth factor-I secretion.Leukemia. 2007, 21(5): 886-896.

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