| 货号 | 11036-1mg |
| 描述 | Geldanamycin (Item No. 13355) is a potent inhibitor of Hsp90 that has poor water solubility. 17-DMAG is a water-soluble derivative of geldanamycin which potently inhibits Hsp90 (IC50 = 24 nM) and has excellent bioavailability and tissue distribution in animals.1 Like other Hsp90 inhibitors, 17-DMAG has diverse anti-tumor actions and has potential in treating certain types of cancer.2,3,4,5,6 This compound also suppresses inflammation by interfering with signaling through the NF-κB pathway.7,8 17-DMAG also ameliorates high fat diet-induced renal failure in a mouse model of diabetes.9 |
| 别名 | Alvespimycin;KOS-1022;NSC 707545; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Egorin, M.J.,Lagattuta, T.F.,Hamburger, D.R., et al. Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats. Cancer Chemotherapy and Pharmacology 49, 7-19 (2002). 2.Bull, E.E.A.,Dote, H.,Brady, K.J., et al. Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin. Clinical Cancer Research 10, 8077-8084 (2004). 3.Taldone, T.,Sun, W. and Chiosis, G. Discovery and development of heat shock protein 90 inhibitors. Bioorganic & Medicinal Chemistry 17(6), 2225-2235 (2009). 4.Hackl, C.,Lang, S.A.,Moser, C., et al. Activating transcription factor-3 (ATF3) functions as a tumor suppressor in colon cancer and is up-regulated upon heat-shock protein 90 (Hsp90) inhibition. BMC Cancer 10(668), 1-9 (2010). 5.Ramanathan, R.K.,Egorin, M.J.,Erlichman, C., et al. Phase I pharmacokinetic and pharmacodynamic study of 17-dimethylaminoethylamino-17-demethoxygeldanamycin, an inhibitor of heat-shock protein 90, in patients with advanced solid tumors. Journal of Clinical Oncology 28(9), 1520-1526 (2010). 6.Kobayashi, N.,Toyooka, S.,Soh, J., et al. The anti-proliferative effect of heat shock protein 90 inhibitor, 17-DMAG, on non-small-cell lung cancers being resistant to EGFR tyrosine kinase inhibitor. Lung Cancer 75, 161-166 (2012). 7.Madrigal-Matute, J.,López-Franco, O.,Blanco-Colio, L.M., et al. Heat shock protein 90 inhibitors attenuate inflammatory responses in atherosclerosis. Cardiovascular Research 86, 330-337 (2010). 8.Shimp, S.K., III,Parson, C.D.,Regna, N.L., et al. HSP90 inhibition by 17-DMAG reduces inflammation in J774 macrophages through suppression of Akt and nuclear factor-κB pathways. Inflammation Research 1-13 (2012). 9.Zhang, H.M.,Dang, H.,Kamat, A., et al. Geldanamycin derivative ameliorates high fat diet-induced renal failure in diabetes. PLoS One 7(3), 1-9 (2012). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 616.8 |
| 分子式 | C32H48N4O8 |
| CAS号 | 467214-20-6 |
| 稳定性 | ≥ 1 year |
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