17-DMAG是Hsp90的抑制劑，IC50值為62±29nm[1]。 17-DMAG可以與Hsp90的ATP結(jié)合基序結(jié)合，并抑制Hsp90的蛋白伴侶活性。它將導(dǎo)致Hsp90的客戶蛋白，如EGFR、AKT、突變型p53和IKK的錯(cuò)誤折疊和隨后的降解。由于在腫瘤細(xì)胞中17-DMAG結(jié)合需要更特異的構(gòu)象Hsp90，并且Hsp90的許多客戶蛋白有助于腫瘤細(xì)胞生長，因此17-DMAG對腫瘤細(xì)胞的毒性通常大于對正常細(xì)胞的毒性[2]。

產(chǎn)品性質(zhì)：

Cas No.:467214-21-7

別名:阿螺旋霉素鹽酸鹽; 17-DMAG hydrochloride; KOS-1022; BMS 826476

化學(xué)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

儲存條件:Store at -20°C

注意事項(xiàng)：

為了您的安全和健康，請穿實(shí)驗(yàn)服并戴一次性手套操作。

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.