ChemicalBook > CAS DataBase List > TAS-116

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
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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)
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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.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0009135
Product name
TAS-116
Purity
98.96%
Packaging
5mg
Price
$85
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
INB0004535
Product name
TAS-116
Purity
95.00%
Packaging
5MG
Price
$503.05
Updated
2021/12/16
ChemScene
Product number
CS-0009135
Product name
TAS-116
Purity
98.96%
Packaging
50mg
Price
$530
Updated
2021/12/16
ChemScene
Product number
CS-0009135
Product name
TAS-116
Purity
98.96%
Packaging
100mg
Price
$940
Updated
2021/12/16
ChemScene
Product number
CS-0009135
Product name
TAS-116
Purity
98.96%
Packaging
10mg
Price
$1450
Updated
2021/12/16
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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

TargetValue
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

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TAS-116 Suppliers

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1260533-36-5, TAS-116Related Search:


  • 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
  • TAS-116
  • 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
  • 1260533-36-5
  • C25H26N8O