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Biological Activity:
Highly potent and oral inhibitor of heat shock protein 90 (Hsp90) in vitro and in vivo, with IC50=21 nM in Hsp90 FP binding assay; inhibits proliferation of various human cancer cell lines in vitro, with GI50 average 9 nM.
References:
MR Jensen et al. NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res. 2008, 10, R33. [online]
SA Eccles et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Res. 2008, 68, 2850. [online]
PA Brough et al. 4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer. J. Med. Chem., 2008, 51 (2), pp 196–218. [online]
T Taldone et al. Targeting Hsp90: small-molecule inhibitors and their clinical development. Cur. Opin. Pharmacol. 2008, 8(4), 370-374. [online]
Chemical Name:
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