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Ganetespib (STA-9090)

Catalog No.
A4385
Hsp90 inhibitor,non-geldanamycin
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
Evaluation Sample
$30.00
In stock
5mg
$50.00
In stock
10mg
$70.00
In stock
50mg
$209.00
In stock
200mg
$500.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Ganetespib (STA-9090; CAS 888216-25-9) is a small-molecule inhibitor targeting heat shock protein 90 (Hsp90). It binds competitively to the ATP-binding pocket located at the N-terminal region of Hsp90, disrupting its chaperone activity and subsequently causing degradation of client proteins involved in tumor growth and survival. Structurally distinct from geldanamycin-derived inhibitors, Ganetespib features a triazolone moiety. Preclinical studies have demonstrated antitumor activity across various cancer cell types, including lung, prostate, colon, breast cancers, melanoma, and leukemia, highlighting its therapeutic potential for cancer research.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt364.4
Cas No.888216-25-9
FormulaC20H20N4O3
SynonymsSTA9090, STA 9090
Solubilityinsoluble in H2O; ≥18.22 mg/mL in DMSO; ≥6.4 mg/mL in EtOH with gentle warming and ultrasonic
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
SDFDownload SDF
Canonical SMILESCC(C)C1=CC(=C2NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)C)C(=O)C=C1O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

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.

Reaction Conditions

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.

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          

Quality Control

Chemical structure

Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

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Ganetespib (STA-9090)

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Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)

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Ganetespib (STA-9090)

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Ganetespib (STA-9090)

Related Biological Data

Ganetespib (STA-9090)