Alvespimycin Chemical Properties

Melting point:

>270°C (dec.)

Boiling point:

810.5±65.0 °C(Predicted)

Density 

1.20

storage temp. 

Desiccate at -20°C

solubility 

DMSO (Slightly), Methanol (Slightly)

form 

Solid

pka

8.48±0.70(Predicted)

color 

Very Dark Purple

Safety Information

HS Code 

29419090

Alvespimycin Usage And Synthesis

Description

Geldanamycin 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. Like other Hsp90 inhibitors, 17-DMAG has diverse anti-tumor actions and has potential in treating certain types of cancer. This compound also suppresses inflammation by interfering with signaling through the NF-κB pathway. 17-DMAG also ameliorates high fat diet-induced renal failure in a mouse model of diabetes.

Chemical Properties

Solid

Uses

17-DMAG is an analogue of Gelamycin (G304500) and 17-(Allylamino)geldanamycin (A549650). 17-DMAG acts as a Hsp90 inhibitor and displays more potent antitumor activity than 17-AAG.

Uses

The labelled derivative of the analogue of Gelamycin (G304500) and 17-(Allylamino)geldanamycin (A549650). It acts as a Hsp90 inhibitor and displays more potent antitumor activity than 17-AAG.

Uses

17-DMAG is a synthetic Geldanamycin derivative and inhibitor of Hsp90.

Definition

ChEBI: A 19-membered macrocyle that is geldanamycin in which the methoxy group attached to the benzoquinone moiety has been replaced by a 2-(N,N-dimethylamino)ethylamino group.

Biological Activity

Water-soluble analog of 17-AAG (17-Demethoxy-17-(2-propenylamino)geldanamycin ) and geldanamycin (9,13-Dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-2-azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione, 9-carbamate ). Binds the ATP binding site of Hsp90 and inhibits its chaperone activity. Displays more potent antitumor activity than 17-AAG (mean GI 50 values are 53 and 123 nM for 17-DMAG and 17-AAG respectively).

Alvespimycin(467214-20-6)Related Product Information

• N,N-Dimethylformamide
• 3-Dimethylaminopropylamine
• Spiramycin
• N,N-Dimethylacetamide
• N,N-Dimethyl-1,4-phenylenediamine
• Dimethyl sulfone
• Ethyl propiolate
• Ethyl acrylate
• Acetylspiramycin
• Dimethyl sulfoxide
• Poly(dimethylsiloxane)
• ISOXADIFEN-ETHYL
• Trinexapac-ethyl
• Ethylparaben
• Ethyl cyanoacetate
• Ethyl acetate
• Ethanol
• 17-DMAG