Specifications
Chemical identification
Synonyms:
- 17-DMAG HCl
- Alvespimycin HCl
- 17-Dimethylaminoethylamino-17-demethoxygeldanamycin Hydrochloride
IUPAC Name:
[(4E,6E,9S,10E,12S,13R,16R)-19-[2-(dimethylamino)ethylamino]-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl] carbamate;hydrochloride
RTECS: LX8922000
17-DMAG, also known as Alvespimycin, is a semisynthetic derivate of Geldanamycin, of less hepatotoxicity, improved water solubility.
17-DMAG is an ansamycin antibiotic which binds to Hsp90 (Heat Shock Protein 90) and alters it function.
Further Information
DMSO, Methanol, Ethanol
- Benzoquinone ansamycin class antibiotic
- Geldanamycin derivate
- HSP90 inhibitor
HSP-90 inhibitor; potential anti-cancer drug
Composition
Supply related information
Publications
Organ-specific efficacy of HSP90 inhibitor in multiple-organ metastasis model of chemorefractory small cell lung cancer.
Takeuchi S, Fukuda K, Arai S, Nanjo S, Kita K, Yamada T, Hara E, Nishihara H, Uehara H, Yano S.
Int J Cancer. 2015 Sep 17. doi: 10.1002/ijc.29858.
PMID: 26379118
P-glycoprotein confers acquired resistance to 17-DMAG in lung cancers with an ALK rearrangement.
Kim HJ, Lee KY, Kim YW, Choi YJ, Lee JE, Choi CM, Baek IJ, Rho JK, Lee JC.
BMC Cancer. 2015 Jul 29;15(1):553. doi: 10.1186/s12885-015-1543-z.
PMID: 26219569
Rapid externalization of 27-kDa heat shock protein (HSP27) and atypical cell death in neutrophils treated with the sphingolipid analog drug FTY720.
Skrzeczyńska-Moncznik J, Bzowska M, Nogieć A, Sroka A, Zarębski M, Vallières L, Guzik K.
J Leukoc Biol. 2015 Jul 27. pii: jlb.3VMA1114-522RR. [Epub ahead of print]
PMID: 26216939
PU-H71: An improvement on nature's solutions to oncogenic Hsp90 addiction.
Trendowski M.
Pharmacol Res. 2015 Sep;99:202-16. doi: 10.1016/j.phrs.2015.06.007. Epub 2015 Jun 25. Review.
PMID:26117427
Targeting HSP90 Ameliorates Nephropathy and Atherosclerosis Through Suppression of NF-κB and STAT Signaling Pathways in Diabetic Mice.
Lazaro I, Oguiza A, Recio C, Mallavia B, Madrigal-Matute J, Blanco J, Egido J, Martin-Ventura JL, Gomez-Guerrero C.
Diabetes. 2015 Oct;64(10):3600-13. doi: 10.2337/db14-1926. Epub 2015 Jun 26.
PMID: 26116697
Heat shock protein 90 inhibitor regulates necroptotic cell death via down-regulation of receptor interacting proteins.
Park SY, Shim JH, Chae JI, Cho YS.
Pharmazie. 2015 Mar;70(3):193-8.
PMID: 25980180
Co-inhibition effect of 17-DMAG and oxaliplatin on proliferation and invasion of colorectal cancer cells.
Zhou J, Wang W, Deng J, Zhou Y, Wu L, Guo Z, Shi J, Shi J, Zhou S, Xu Z.
Zhonghua Wei Chang Wai Ke Za Zhi. 2015 Apr;18(4):370-5. Chinese.
PMID: 25940182
The HSP90 inhibitor alvespimycin ( 17-DMAG ) enhances the potency of telomerase inhibition by imetelstat in human osteosarcoma.
Hu Y, Bobb D, He J, Hill DA, Dome JS.
Cancer Biol Ther. 2015;16(6):949-57. doi: 10.1080/15384047.2015.1040964. Epub 2015 Apr 28.
PMID: 25920748
Molecular chaperone Hsp90 is a therapeutic target for noroviruses.
Vashist S, Urena L, Gonzalez-Hernandez MB, Choi J, de Rougemont A, Rocha-Pereira J, Neyts J, Hwang S, Wobus CE, Goodfellow I.
J Virol. 2015 Jun;89(12):6352-63. doi: 10.1128/JVI.00315-15. Epub 2015 Apr 8.
PMID: 25855731