17-DMAG Inhibitor CAS No. 467214-20-6

Cat. No.	Name	Size	Price
KI0162	17-DMAG	5 mg	$192
	17-DMAG	10 mg	$473.6
	17-DMAG	50 mg	$729.6

Chemical Characteristic

Product Name	17-DMAG
Synonyms	KOS-1022, alvespimycin
CAS No.	467214-20-6
Molecular Weight	616.75
Formula	C₃₂H₄₈N₄O₈
Chemical Name	[(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
Smiles	C(=O)(N)OC1/C(=C/[C@@H]([C@H]([C@H](C[C@@H](CC2=C(C(=O)C=C(NC(=O)/C(=C/C=C\[C@@H]1OC)/C)C2=O)NCCN(C)C)C)OC)O)C)/C
Chemical Structure

Biological activities

17-DMAG is a potent HSP90 inhibitor. The EC50 of 17-DMAG binding Hsp90 is 62 nM. In contrast, The EC50 of 17-DMAG is 65 nM against Grp94 (94 kDa glucose regulated protein). The GI50 of 17-DMAG is 29 and 32 nM against SKBR3 and SKOV3 cells, respectively. However, the EC50 of 17-DMAG for Hsp70 induction in SKBR3 and SKOV3 cells is 4 and 14 nM, respectively. ^[1] SKOV-3 cells are sensitive to 17-DMAG treatment, in a dose-dependent manner, with an IC50 of 24.72 nM after 72 hours incubation.^[2] 17-DMAG treatment also inhibits FGF-2 and VEGF-induced HUVEC proliferation and results in apoptosis. 17-DMAG consistently increases the expression of Hsp70. ^[3] The IC50 of 17-DMAG for some EGFR-mutant cell lines including eight EGFR-TKI resistant cell lines (such as NCI-H3255 and PC-9 cells) ranges from 0.04 to 0.16 µM while those for seven EGFR-wild type cell lines (such as HCC15 cells) ranges from 1.6 to 27.4 µM.^[4] In mice xenograft models, 17-DMAG significantly reduces the growth of EGFR-mutant lines irrespective of T790M mutation.^[4] Administration of 17-DMAG markedly ameliorates motor impairments in SBMA mice without detectable toxicity and reduces amounts of monomeric and nuclear-accumulated mutant AR (androgen receptor). Mutant AR is preferentially degraded in the presence of 17-DMAG in both SBMA cell and mouse models when compared with wild-type AR.^[5]

References

[1] Ge J, et al. 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(15): 4606-4615. [2] Niu G, et al. Monitoring therapeutic response of human ovarian cancer to 17-DMAG by noninvasive PET imaging with 64Cu-DOTA-trastuzumab. Eur J Nucl Med Mol Imaging. 2009, 36(9): 1510-1519. [3] Kaur G, et al. Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator. Clin Cancer Res. 2004, 10(14): 4813-4821. [4] Kobayashi N, 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. 2012, 75(2): 161-166. [5] Tokui K, et al. 17-DMAG ameliorates polyglutamine-mediated motor neuron degeneration through well-preserved proteasome function in an SBMA model mouse. Hum Mol Genet. 2009, 18(5): 898-910.

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