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17-DMAG

BVT-0255-C100 100 µg INQ
BVT-0255-M001 1 mg INQ
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Additional Information

Product Data
Synonyms NSC 707545; 17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin
Properties
Formula C32H48N4O8
MW 616.8
CAS 467214-20-6
Source/Host Semi-synthetic derivative from geldanamycin.
Purity ≥98% (HPLC)
Appearance Purple to black powder.
Solubility Soluble in water, 100% ethanol (10 mg/ml) or DMSO (>25 mg/ml)
Identity Determined by 1H-NMR.
Origin Manufactured by BioViotica.
InChi Key KUFRQPKVAWMTJO-LMZWQJSESA-N
Product Type Chemical
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Protect from light when in solution.
Use/Stability Stable for at least 1 year after receipt when stored at -20°C. After reconstitution protect from light at -20°C.
Documents
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Product Description

  • Less toxic, more potent synthetic derivative of geldanamycin (Prod. No. BVT-0196).
  • Angiogenesis inhibitor.
  • Heat shock protein 90 (HSP90) inhibitor.
  • Apoptosis inducer.
  • Shows higher antitumor activity than 17-AAG (Prod. No. BVT-0244).

Product References

  1. Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats: M.J. Egorin, et al.; Cancer Chemother. Pharmacol. 49, 7 (2002)
  2. Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats: S.M. Musser, et al.; Cancer Chemother. Pharmacol. 52, 139 (2003)
  3. Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90: J.M. Jez, et al.; Chem. Biol. 10, 361 (2003)
  4. Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator: G. Kaur, et al.; Clin. Cancer Res. 10, 4813 (2004)
  5. Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: E.E. Bull, et al.; Clin. Cancer Res. 10, 8077 (2004)
  6. Synthesis and biological activities of novel 17-aminogeldanamycin derivatives: Z.Q. Tian, et al.; Bioorg. Med. Chem. 12, 5317 (2004)
  7. 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: V. Smith, et al.; Cancer Chemother. Pharmacol. 56, 126 (2005)
  8. In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative: M. Hollingshead, et al.; Cancer Chemother. Pharmacol. 56, 115 (2005)
  9. Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance: E.R. Glaze, et al.; Cancer Chemother. Pharmacol. 56, 637 (2005)
  10. Structure-based design of 7-carbamate analogs of geldanamycin: G. Rastelli, et al.; Biooorg. Med. Chem. Lett. 15, 5016 (2005)
  11. Determination of the heat shock protein 90 inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin in plasma by liquid chromatography-electrospray mass spectrometry: K. Hwang, et al.; J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 830, 35 (2006)
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