Alvespimycin HCl, also known as 17-DMAG, is a potent, water-soluble HSP90 inhibitor. Alvespimycin has diverse anti-tumor actions and has potential in treating a number of different types of cancers, including ovarian, prostate, melatnoma, non-small-cell lung cancer, and several leukemias (chronic lymphocytic, acute myeloid). This compound also suppresses inflammation by interfering with signaling through the NF-κB pathway.
≥26.2 mg/ml in DMSO; insoluble in EtOH; ≥3.04 mg/mL in H2O For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Long-term storage in solution is not recommended. Not stable in diluted solutions.
Biological Activity
17-DMAG is an inhibitor of Hsp90 with IC50 value of 62±29 nM.
CAS Registry #
467214-21-7
Background
Alvespimycin hydrochloride is the hydrochloride salt of alvespimycin, an analogue of the antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction.
References
1. Smith V et al. Cancer Chemother Pharmacol. 2005 Aug;56(2):126. 2. Lancet JE, et al. 2010 Apr;24(4):699-705.
Storage/Stability
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.