NVP-AUY922 is a resorcinol-based, intravenous or intraperitoneal Phase II clinical trial HSP90 inhibitor with a Kd of 1.7 nM. It inhibits tumor cell proliferation at GI50 values of 2-40 nM, inducing G1-G2 arrest and apoptosis. [1] Daily dosing of NVP-AUY922 (50 mg/kg, iv or ip) produced statistically significant tumor inhibition or regression (treated/control) in BT474 breast, 21%; A2780 ovarian, 11%; U87MG glioblastoma, 7%; PC3 prostate, 37%; and WM266.4 melanoma, 31%. [1]
Pharmacodynamically, NVP-AUY922 induces HSP70 and depletes ERBB2, CRAF, CDK4, phospho-AKT/TotalAKT, and HIF-1a.
Technical information:
| Chemical Formula: | C26H31N3O5 | |
| CAS #: | 747412-49-3 | |
| Molecular Weight: | 465.54 | |
| Purity: | >99% | |
| Appearance: | White | |
| Chemical Name: | 5-(2,4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | NVP-AUY-922; AUY922; VER-52296. Ver52296 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Eccles et al., NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. Cancer Res. 2008, 68, 2850-2860. Pubmed ID: 18413753 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
