AUY-922, also known as Luminespib, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines.
Chemical Formula: C26H31N3O5
Exact Mass: 465.22637
Molecular Weight: 465.54
Elemental Analysis: C, 67.08; H, 6.71; N, 9.03; O, 17.18
Appearance: White to light yello solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Luminespib is a potent and selective HSP90 inhibitor, with IC50s and Kis of 21 ± 16, 8.2 ± 0.7 nM against HSP90β and of 7.8 ± 1.8, 9.0 ± 5.0 nM for HSP90α. Luminespib shows weak activity against GRP94 and TRAP-1 wich IC50s of 535 ± 51 nM (Ki, 108 nM) and 85 ± 8 nM (Ki, 53 nM), respectively. Luminespib exhibits inhibitory effect on proliferation of various human tumor cell lines (2.3-49.6 nM), induces cell cycle arrest and apoptosis and depletes client proteins in human cancer cells (80 nM). Luminespib (100 nM) significantly reduces CD40L fibroblast-induced changes in immunophenotype and STAT3 signaling but with no effect on the viability of chronic lymphocytic leukemia (CLL) cells. Luminespib (500 nM) in combination with NSC 118218 more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor. Luminespib shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. Luminespib (10 nM) reduces the expression and the epidermal growth factor (EGF)-mediated activation of EGFR and substantially disrupts EGF signaling in terms of diminishing downstream phosphorylation of ERKThr202/Tyr204. Luminespib (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF.
Luminespib (50, 75 mg/kg, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11 in human tumor xenografts. Luminespib (50 mg/kg/week, 3×25 mg/kg/week) significantly reduces tumor growth rates and lowers tumor weights in the L3.6pl pancreatic cancer cell-bearing mice model.
Gaykema SB, SchrÃ¶der CP, Vitfell-Rasmussen J, Chua S, Oude Munnink TH, Brouwers AH, Bongaerts AH, Akimov M, Fernandez-Ibarra C, Lub-de Hooge MN, de Vries EG, Swanton C, Banerji U. 89Zr-trastuzumab and 89Zr-bevacizumab PET to Evaluate the Effect of the HSP90 Inhibitor NVP-AUY922 in Metastatic Breast Cancer Patients. Clin Cancer Res. 2014 Aug 1;20(15):3945-54. doi: 10.1158/1078-0432.CCR-14-0491. PubMed PMID: 25085789.
Doi T, Onozawa Y, Fuse N, Yoshino T, Yamazaki K, Watanabe J, Akimov M, Robson M, Boku N, Ohtsu A. Phase I dose-escalation study of the HSP90 inhibitor AUY922 in Japanese patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Sep;74(3):629-36. doi: 10.1007/s00280-014-2521-x. Epub 2014 Jul 25. PubMed PMID: 25059319; PubMed Central PMCID: PMC4143601.
Chiang NJ, Wu SN, Kao CA, Huang YM, Chen LT. Stimulation of Electroporation-Induced Inward Currents in Glioblastoma Cell Lines by the Heat Shock Protein Inhibitor AUY922. Clin Exp Pharmacol Physiol. 2014 Jun 7. doi: 10.1111/1440-1681.12273. [Epub ahead of print] PubMed PMID: 24909268.
Huang J, Sun C, Zhang T, Pan L, Wang S, He Q, Li D. Potent antitumor activity of HSP90 inhibitor AUY922 in adrenocortical carcinoma. Tumour Biol. 2014 May 22. [Epub ahead of print] PubMed PMID: 24850175.
Chen SM, Guo CL, Shi JJ, Xu YC, Chen Y, Shen YY, Su Y, Ding J, Meng LH. HSP90 inhibitor AUY922 abrogates up-regulation of RTKs by mTOR inhibitor AZD8055 and potentiates its antiproliferative activity in human breast cancer. Int J Cancer. 2014 Apr 7. doi: 10.1002/ijc.28880. [Epub ahead of print] PubMed PMID: 24706460.
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