Dimethylaminoethylamino-17-demethoxygeldanamycin, 17-

Dimethylaminoethylamino-17-demethoxygeldanamycin, 17-

$255.00 - 1 mg

$895.00 - 5 mg

All prices in Australian dollars

Code
BIA-D1924
Synonyms
Alvespimycin, DMAG, NSC 707545, 17-DMAG
CAS #
467214-20-6
Molecular Formula
C32H48N4O8
Molecular Weight
616.75
Purity
>95% by HPLC
Long Term Storage
-20°C
Solubility
Soluble in methanol or DMSO

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Product Data Sheet

Application Notes

17-Dimethylaminoethylamino-17-demethoxygeldanamycin (DMAG, alvespimycin) is a semi-synthetic derivative of the benzoquinone ansamycin antibiotic isolated from Streptomyces hygroscopicus in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group. DMAG acts by binding to the 90-kDa heat shock protein (Hsp90) essential to maintain the conformation, stability, activity and cellular localisation of several key oncogenic proteins such as ERBB2, C-RAF, CDK4, AKT/PKB, steroid hormone receptors, mutant p53, HIF-1α, survivin and telomerase hTERT. DMAG is more potent than geldanamycin and 17-allylamino-17-demethoxygeldanamycin (17AAG) as an inhibitor of Hsp90.

References

  • Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90. Schneider C. et al., Proc Natl Acad Sci. 1996, 93, 14536.
  • Mechanistic studies on Hsp90 inhibition by ansamycin derivatives. Onuoha S.C. et al. J Mol Biol. 2007, 372, 287.  
  • Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models. Smith V. et al. Cancer Chemother Pharmacol. 2005, 56, 126.

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