Catalog No. size PriceQuantity
M6487-2 2mg solid $98
M6487-10 10mg solid $406


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 AUY-922 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.

Product information

CAS Number: 747412-49-3

Molecular Weight: 465.54

Formula: C26H31N3O5


AUY 922








VER 52296

Chemical Name: 5-(2,4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide

Smiles: CCNC(=O)C1=NOC(=C1C1=CC=C(CN2CCOCC2)C=C1)C1=CC(C(C)C)=C(O)C=C1O


InChi: InChI=1S/C26H31N3O5/c1-4-27-26(32)24-23(18-7-5-17(6-8-18)15-29-9-11-33-12-10-29)25(34-28-24)20-13-19(16(2)3)21(30)14-22(20)31/h5-8,13-14,16,30-31H,4,9-12,15H2,1-3H3,(H,27,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

AUY-922 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. AUY-922 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. AUY-922 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). AUY-922 (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. AUY-922 (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. AUY-922 shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. AUY-922 (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. AUY-922 (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF.

In Vivo:

AUY-922 (50, 75 mg/kg, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11 in human tumor xenografts. AUY-922 (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.


  1. 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.
  2. 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.
  3. 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.

Products are for research use only. Not for human use.

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