Search Site
Home >> Signaling Pathways >> Proteases >> HSP >> Ganetespib (STA-9090)
Related Products
Ganetespib (STA-9090)Hsp90 inhibitor,non-geldanamycin

Ganetespib (STA-9090)

Catalog No. A4385
Size Price Stock Qty
10mM (in 1mL DMSO) $150.00 In stock
Evaluation Sample $28.00 In stock
5mg $135.00 In stock
10mg $187.00 In stock
50mg $550.00 In stock
200mg $1,650.00 In stock

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

Biological Activity

Description Ganetespib (STA-9090) is an inhibitor of HSP90 with IC50 of 4 nM in OSA 8 cells.
Targets HSP90          
IC50 4 nM          

Protocol

Cell experiment [1]:

Cell lines

NCI-H1975 and HCC827 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reacting condition

0.001 ~ 1 μM; 5, 15 or 60 mins or 24 hrs

Applications

In NCI-H1975 and HCC827 cells, exposure to Ganetespib for only 60 mins resulted in cytotoxicity with IC50 values of 510 and 800 nM, respectively. In NCI-H1975 cells, a 5-minute exposure to Ganetespib still resulted in an IC50 value < 1 μM.

Animal experiment [1]:

Animal models

SCID mice bearing NCI-H1395 NSCLC xenografts

Dosage form

150 mg/kg; i.v.; once weekly

Applications

Ganetespib induced NCI-H1395 tumor regression, with a T/C value of -49%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Weiwen Ying, Zhenjian Du, Lijun Sun, Kevin P. Foley, David A. Proia, Ronald K. Blackman, Dan Zhou, Takayo Inoue, Noriaki Tatsuta, Jim Sang, Shuxia Ye, Jamie Acquaviva, Luisa Shin Ogawa, Yumiko Wada, James Barsoum, and Keizo Koya. Ganetespib, a unqiue triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther 2012; 11: 475-484.

Ganetespib (STA-9090) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Ganetespib (STA-9090) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 888216-25-9 SDF Download SDF
Synonyms STA9090, STA 9090
Chemical Name (5Z)-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-(1-methylindol-5-yl)-1,2,4-triazolidin-3-one
Canonical SMILES CC(C)C1=CC(=C2NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)C(=O)C=C1O
Formula C20H20N4O3 M.Wt 364.4
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Ganetespib (also known as STA-9090), 5-[2,4-dihydroxy-5-(1 methylethyl)phenyl]-2,4 dihydro-4-(1-methyl-1H indol-5 yl)-3H-1,2,4 triazole-3-one, is a potent small-molecule inhibitor of heat shock protein 90 (Hsp90), which binds to the ATP pocket in the N-terminus of Hsp90 resulting in down-regulation of Hsp90 client protein levels. Being structurally unrelated to geldanamycin-derived Hsp90 inhibitors (17-AAG, 17-DMAG, and IPI-504), ganetespib has a unique triazolone-containing chemical structure and stands out other Hsp90 inhibitors in terms of potency, antitumor activity, and safety profile. Results of previous studies indicate that ganetespib exhibits antitumor activity against a broad range of human cancers, including lung cancer, prostate cancer, colon cancer, breast cancer, melanoma and leukemia.

Reference

Weiwen Ying, Zhenjian Du, Lijun Sun, Kevin P. Foley, David A. Proia, Ronald K. Blackman, Dan Zhou, Takayo Inoue, Noriaki Tatsuta, Jim Sang, Shuxia Ye, Jamie Acquaviva, Luisa Shin Ogawa, Yumiko Wada, James Barsoum, and Keizo Koya. Ganetespib, a unqiue triazolone-containing Hsp90 inhibitor, exhibits potent antitumor activity and a superior safety profile for cancer therapy. Mol Cancer Ther 2012; 11: 475-484

Jonathan W Goldman, Robert N Raju, Gregory A Gordon, Iman El-Hariry, Florentina Teofilivivi, Vojo M Vukovic, Robert Bradley, Michael D Karol, Yu Chen, Wei Guo, Takayo Inoue and Lee Rosen. A first in human, safety, pharmacokinetics, and clinical activity phase I study of once weekly administration of the Hsp90 inhibitor ganetespib (STA-9090) in patients with solid malignancies. BMC Cancer 2013; 13:152