17-DMAG是Hsp90的抑制剂，IC50值为62±29nm[1]。 17-DMAG可以与Hsp90的ATP结合基序结合，并抑制Hsp90的蛋白伴侣活性。它将导致Hsp90的客户蛋白，如EGFR、AKT、突变型p53和IKK的错误折叠和随后的降解。由于在肿瘤细胞中17-DMAG结合需要更特异的构象Hsp90，并且Hsp90的许多客户蛋白有助于肿瘤细胞生长，因此17-DMAG对肿瘤细胞的毒性通常大于对正常细胞的毒性[2]。

产品性质：

Cas No.:467214-21-7

别名:阿螺旋霉素盐酸盐; 17-DMAG hydrochloride; KOS-1022; BMS 826476

化学名: [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-21-[2-(dimethylamino)ethylamino]-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate;hydrochloride

Canonical SMILES: CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)C)OC)OC(=O)N)C)C)O)OC.Cl

分子式:C32H48N4O8.HCl

分子量:653.21

溶解度:≥ 26.2mg/mL in DMSO

储存条件:Store at -20°C

注意事项：

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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 efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative. Cancer Chemother Pharmacol. 2005, 56: 115–125.