Loading... Please wait...

Categories

Our Newsletter


TAS-116

  • Image 1
Price:
$129.00
Catalog #:
C8271
Quantity:


Product Description

TAS-116 is an orally bioavailable HSP90 inhibitor that showed potent anti-tumor activity in many in vitro and in vivo models. TAS-116 is a selective inhibitor of cytosolic HSP90? and ? that does not inhibit HSP90 paralogs such as endoplasmic reticulum GRP94 or mitochondrial TRAP1 [1]. Multiple clinical trials are on-going testing the synergistic anti-tumor effect of combined therapy strategy with TAS-116 for treatment of advanced solid tumors. TAS-116 has a potential to enhancing antitumor activity while minimizing adverse effects that are observed with other compounds of this class [2,3].


Technical information:

Chemical Formula:   C25H26N8O
CAS #:   1260533-36-5
Molecular Weight:   454.53
Purity:   > 98%
Appearance:   White
Chemical Name:   3-ethyl-4-(3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl)benzamide
Solubility:   Up to 275 mM in DMSO
Synonyms:   TAS 116, TAS116

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


Reference:

1. Ohkubo S, et al. TAS-116, a Highly Selective Inhibitor of Heat Shock Protein 90? and ?, Demonstrates Potent Antitumor Activity and Minimal Ocular Toxicity in Preclinical Models. Mol Cancer Ther 2014; 14(1): 14–22. Pubmed ID: 25416789
2. Shimomura A, et al. First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors. Mol Cancer Ther. 2019; 18(3):531-540 Pubmed ID: 30679388
3. Kawazoe A, et al. TAS-116, an oral HSP90 inhibitor, in combination with nivolumab in patients with colorectal cancer and other solid tumors: An open-label, dose-finding, and expansion phase Ib trial (EPOC1704). J Clin Oncol 2020; 38 (15) suppl:4044 Pubmed ID: DOI: 10.1200/JCO.2020.38.15_suppl.4044

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Find Similar Products by Category

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the TAS-116 to your wish list.

You Recently Viewed...