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| | TAS-116 Basic information |
| Product Name: | TAS-116 | | Synonyms: | TAS-116;TAS 116;TAS116;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;Benzamide, 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]-;Des-iPr-TAS-116;Pimitespib (TAS-116);Pimitespib;inhibit,HSP,TAS 116,TAS116,Pimitespib,Heat shock proteins,Inhibitor | | CAS: | 1260533-36-5 | | MF: | C25H26N8O | | MW: | 454.53 | | EINECS: | | | Product Categories: | | | Mol File: | 1260533-36-5.mol |  |
| | TAS-116 Chemical Properties |
| Boiling point | 661.7±55.0 °C(Predicted) | | density | 1.36±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: soluble | | form | A solid | | pka | 15.43±0.50(Predicted) | | color | White to off-white |
| | TAS-116 Usage And Synthesis |
| Biological Activity | TAS-116 is a novel small molecule inhibitor of HSP90 with Ki values of 34.7 nmol/L and 21.3 nmol/L for HSP90α and HSP90β, respectively. It does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). | | in vitro | TAS-116 is a selective inhibitor of HSP90α and HSP90β in the cytoplasm, but has no inhibitory effect on endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μM of TAS-1116 for 8 hours resulted in a decrease in DDR1 levels and induction of HSP70. | | in vivo | In a mouse model with human xenograft tumors, oral administration of TAS-116 induced tumor shrinkage accompanied by depletion of HSP90. In a rat model, TAS-116 was more distributed in subcutaneously xenografted NCI-H1975 non-small cell lung cancer tumors than in the retina. TAS-116 was also active in orthotopically transplanted NCI-H1975 lung tumors. | | target | | Target | Value | HSP90β
(Cell-free assay) | 21.3 nM(Ki) | HSP90α
(Cell-free assay ) | 34.7 nM(Ki) |
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| | TAS-116 Preparation Products And Raw materials |
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