Alvespimycin HCl (17-DMAG)

Catalog #: 27730-2
Size: 100 mg
$320
MW: 653.2 Da
CAS Registry #: 467214-21-7
Formula: C32H48N4O8 • HCl
Target: HSP90
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.
Description:
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.
Synonym(s):
17-DMAG; KOS-1022; NSC707545; 17-demethoxy-17-[[2-(dimethylamino)ethyl]amino]-geldanamycin
Purity:

≥95% by HPLC

Biological Activity:
Alvespimycin (also known as 17-DMAG) displays ~2 times potency against human Hsp90 than 17-AAG, with IC50 of 62 nM versus 119 nM.
Solubility:
Soluble in DMSO (100 mM). Solubility in water is less than 1 mg/ml (1 mM).
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.

Reference(s):
1. Smith V et al. Cancer Chemother Pharmacol. 2005 Aug;56(2):126.
2. Lancet JE, et al. 2010 Apr;24(4):699-705.
Scientific Category:
HSP Inhibitor
Product Type:
Inhibitor
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