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HomeProduct name listTAS-116

TAS-116

TAS-116 Structural

What is TAS-116?

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.

Properties of TAS-116

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

Safety information for TAS-116

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for TAS-116

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