D-3440 17-DMAG, Hydrochloride Salt, >99%

Synonyms : [Alvespimycin]

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  • M.W. 653.21
  • C32H48N4O8•HCl
  • [467214-21-7]

Warnings: Toxic.

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO; soluble up to about 2 mg/mL in water. Disposal: A.

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  • Synthetic derivative of geldanamycin, Cat. No. G-4500, and water-soluble analog of 17-AAG, Cat. No. A-6880, demonstrating stability and low in vivo toxicity similar to 17-AAG, but undergoes limited metabolism compared to 17-AAG. Egorin, M.J., et al. "Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats." Cancer Chemother. Pharmacol. 49: 7-19 (2002).
  • Binds specifically to heat shock protein Hsp90 in a manner similar to geldanamycin. Tian, Z.Q., et al. "Synthesis and biological activities of novel 17-aminogeldanamycin derivatives." Bioorg. Med. Chem. 12: 5317-5329 (2004).
  • Inhibits angiogenesis. Kaur, G, et al. "Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator." Clin. Cancer Res. 10: 4813-4821 (2004).
  • Enhances the radiation-induced cell cycle arrest of human solid tumor cell lines both in vitro and in vivo. Bull, E.E., et al. "Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin." Clin. Cancer Res. 10: 8077-8084 (2004).
  • Exhibits potent anti-tumor activity against MDA-MB-231 breast carcinoma cells and HL60-TB leukemia cells both of which are relatively insensitive to 17-AAG. Hollingshead, M., et al. "In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative." Cancer Chemother. Pharmacol. 56: 115-125 (2005).
  • Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
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