TAS-116
- Product Name
- TAS-116
- CAS No.
- 1260533-36-5
- Chemical Name
- TAS-116
- Synonyms
- TAS-116;Pimitespib;TAS 116;TAS116;Des-iPr-TAS-116;Pimitespib (TAS-116);inhibit,HSP,TAS 116,TAS116,Pimitespib,Heat shock proteins,Inhibitor;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]-
- CBNumber
- CB22716365
- Molecular Formula
- C25H26N8O
- Formula Weight
- 454.53
- MOL File
- 1260533-36-5.mol
TAS-116 Property
- 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)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0009135
- Product name
- TAS-116
- Purity
- 98.96%
- Packaging
- 5mg
- Price
- $85
- Updated
- 2021/12/16
- Product number
- INB0004535
- Product name
- TAS-116
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $503.05
- Updated
- 2021/12/16
- Product number
- CS-0009135
- Product name
- TAS-116
- Purity
- 98.96%
- Packaging
- 50mg
- Price
- $530
- Updated
- 2021/12/16
- Product number
- CS-0009135
- Product name
- TAS-116
- Purity
- 98.96%
- Packaging
- 100mg
- Price
- $940
- Updated
- 2021/12/16
- Product number
- CS-0009135
- Product name
- TAS-116
- Purity
- 98.96%
- Packaging
- 10mg
- Price
- $1450
- Updated
- 2021/12/16
TAS-116 Chemical Properties,Usage,Production
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) |
TAS-116 Preparation Products And Raw materials
Raw materials
Preparation Products
TAS-116 Suppliers
- Tel
- +1-781-999-5354 +1-00000000000
- marketing@targetmol.com
- Country
- United States
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- +1-708-310-1919 +1-13798911105
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- 708-557-7486
- sales@invivochem.cn
- Country
- United States
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- +1-+1(833)-552-7181
- sales@aladdinsci.com
- Country
- United States
- ProdList
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