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Key Documents

D5193

Sigma-Aldrich

17-Dimethylaminoethylamino-17-demethoxygeldanamycin

Synonym(s):

17-DMAG

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About This Item

Empirical Formula (Hill Notation):
C32H48N4O8
Molecular Weight:
616.75
UNSPSC Code:
51102829
NACRES:
NA.85

biological source

synthetic

Quality Level

form

powder

color

dark red-purple to black

solubility

ethanol: ~10 mg/mL (lit.)
DMSO: >25 mg/mL (lit.)

antibiotic activity spectrum

neoplastics

Mode of action

protein synthesis | interferes

storage temp.

−20°C

General description

Chemical structure: benzenoid

Application

17-DMAG has been used to block the NF-κB inflammatory cascade in the murine model. It a potential therapeutic agent for non-small-cell lung cancers (NSCLC).

Biochem/physiol Actions

17-DMAG is a heat shock protein (HSP90) inhibitor. 17-DMAG is a more potent analog of geldanamycin. It inhibits cancer growth and promotes apoptosis in multiple cell lines. 17-DMAG is a more potent antitumor agent than 17-AAG.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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HSP90 inhibition by 17-DMAG reduces inflammation in J774 macrophages through suppression of Akt and nuclear factor-κB pathways.
Shimp SK 3rd, Parson CD, et al.
Inflammation Research, epub (2012)
Naruyuki Kobayashi et al.
Lung cancer (Amsterdam, Netherlands), 75(2), 161-166 (2011-07-20)
Acquired resistance to epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), gefitinib and erlotinib, is frequently observed after initiation of TKIs therapy. Non-small-cell lung cancers (NSCLC) with activating EGFR mutations were reported to be sensitive to heat shock protein 90 (Hsp90)

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