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17-DMAG (Alvespimycin) HClHsp90 inhibitor

17-DMAG (Alvespimycin) HCl

Catalog No. BCC1175
Size Price Stock
10mM (in 1mL DMSO) $70.00 In stock
10mg $50.00 In stock
25mg $100.00 In stock
100mg $250.00 In stock
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Quality Control of 17-DMAG (Alvespimycin) HCl

Chemical structure

17-DMAG (Alvespimycin) HCl

Biological Activity of 17-DMAG (Alvespimycin) HCl

Water-soluble analog of 17-AAG and geldanamycin. Binds the ATP binding site of Hsp90 and inhibits its chaperone activity. Displays more potent antitumor activity than 17-AAG (mean GI50 values are 53 and 123 nM for 17-DMAG and 17-AAG respectively).

17-DMAG (Alvespimycin) HCl Dilution Calculator

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17-DMAG (Alvespimycin) HCl Molarity Calculator

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Chemical Properties of 17-DMAG (Alvespimycin) HCl

Cas No. 467214-21-7 SDF Download SDF
Synonyms NSC 707545
Chemical Name 17-Demethoxy-17-[[2-(dimethylamino)ethyl]amino]geldanamycin hydrochloride
Formula C32H48N4O8.HCl M.Wt 653.21
Solubility Soluble to 30 mM in DMSO and to 10 mM in ethanol
Storage Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of 17-DMAG (Alvespimycin) HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5309 mL 7.6545 mL 15.309 mL 30.618 mL 38.2725 mL
5 mM 0.3062 mL 1.5309 mL 3.0618 mL 6.1236 mL 7.6545 mL
10 mM 0.1531 mL 0.7655 mL 1.5309 mL 3.0618 mL 3.8273 mL
50 mM 0.0306 mL 0.1531 mL 0.3062 mL 0.6124 mL 0.7655 mL
100 mM 0.0153 mL 0.0765 mL 0.1531 mL 0.3062 mL 0.3827 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Background on 17-DMAG (Alvespimycin) HCl

17-DMAG is an inhibitor of Hsp90 with IC50 value of 62±29nM [1].

17-DMAG can bind to the ATP-binding motif of Hsp90 and inhibit the protein chaperoning activity of Hsp90. It will cause misfolding and subsequent degradation of Hsp90’s client proteins, such as EGFR, AKT, mutant p53, and IKK. Since there are more speci?c conformation Hsp90 required for 17-DMAG binding in tumor cells and many client proteins of Hsp90 contribute to tumor cell growth, 17-DMAG is usually more toxic to tumor cells than to normal cells [2].

17-DMAG is reported as an antitumor agent with more broadly exploitable activity and more pharmaceutically tractable characteristics in the in vitro and initial in vivo assay. 17-DMAG can effect cell growth when treating the NCI 60 cell lines with it, the mean GI50 is 0.053mM. The in vivo activity of 17-DMAG is tested in four melanoma models using the Freiburg human tumor xenograft panel and two lung xenografts. It shows that 17-DMAG has high activity in the two lung xenografts and two of the four melanoma models, but not in another two, MEXF 462 and MEXF 514 [3].

References:
[1] Jie Ge, Emmanuel Normant, James R. Porter, Janid A. Ali, Marlene S. Dembski, Yun Gao, Asimina T. Georges, Louis Grenier, Roger H. Pak, Jon Patterson, Jens R. Sydor, Thomas T. Tibbitts, Jeffrey K. Tong, Julian Adams, and Vito J. Palombella. Design, synthesis and biological evaluation of Hydroquinone derivatives of 17-Amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90. J. Med. Chem. 2006, 49, 4606-4615.
[2] Xiaoping Sun, Jillian A. Bristol, Satoko Iwahori, Stacy R. Hagemeier, Qiao Meng, Elizabeth A. Barlow, Joyce D. Fingeroth, Vera L. Tarakanova, Robert F. Kalejta, Shannon C. Kenney. Hsp90 Inhibitor 17-DMAG Decreases Expression of Conserved Herpesvirus Protein Kinases and Reduces Virus Production in

Epstein-Barr Virus-Infected Cells. Journal of Virology. 2013, 87 (18): 10126–10138.

[3] Melinda Hollingshead, Michael Alley, Angelika M. Burger, Suzanne Borgel,

Christine Pacula-Cox, Heinz-Herbert Fiebig, Edward A. Sausville. In vivo antitumor ef?cacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative. Cancer Chemother Pharmacol. 2005, 56: 115–125.

Kewords:

17-DMAG (Alvespimycin) HCl,467214-21-7,NSC 707545,Metabolism,HSP, supplier, inhibitor,Antagonist,Blocker,Modulator,Agonist, activators, activates, potent, BioCrick

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