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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): 1422. 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.
