TAS-116

For research use only.

Catalog No.S7716

TAS-116 Chemical Structure

Molecular Weight(MW): 454.53

TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).

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Biological Activity

Description TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
Targets
HSP90β [1]
(Cell-free assay)
HSP90α [1]
(Cell-free assay )
21.3 nM(Ki) 34.7 nM(Ki)
In vitro

TAS-116 is a selective inhibitor of cytosolic HSP90α and β that does not inhibit HSP90 paralogs such as endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μmol/L TAS-116 for 8 hours results in reduced levels of DDR1, which interacts with HSP90α and induction of HSP70, which is a surrogate marker of cytosolic HSP90 inhibition[1].

Assay
Methods Test Index PMID
Western blot
p-B-Raf / B-raf / p-C-Raf / C-Raf / p-MEK / MEK / p-ERK / ERK / p-AKT / AKT / PARP; 

PubMed: 26630652     


NCI-H929 and RPMI-8226 cells were treated with the indicated doses of TAS-116 for 24 h. Whole-cell lysates were subjected to western blotting using p-B-Raf, B-Raf, p-C-Raf, C-Raf, p-MEK1/2, MEK1/2, p-ERK, ERK, p-Akt (S473), Akt, PARP, and β-actin Abs. FL, full-length; CF, cleaved form.

26630652
Growth inhibition assay
Cell viability; 

PubMed: 26630652     


NCI-H929, INA6, MM.1S, and RPMI-8226 MM cell lines were cultured with TAS-116 (0–5 μM) for 24, 48, or 72 h. In each case, cell viability was assessed with the MTT assay of triplicate cultures and expressed as the percentage of the untreated control. Data are the mean ± SD.

26630652
In vivo

Oral administration of TAS-116 leads to tumor shrinkage in human tumor xenograft mouse models accompanied by depletion of multiple HSP90 clients. In a rat model, the antitumor activity of TAS-116 is accompanied by a higher distribution of the compound in subcutaneously xenografted NCI-H1975 non-small cell lung carcinoma tumors than in retina. TAS-116 shows activity against orthotopically transplanted NCI-H1975 lung tumors. Pharmacokinetic profiling of TAS-116 in rodent and nonrodent species shows that TAS-116 is orally absorbed and had a bioavailability of almost 100% in mice, 69.0% in rats, and 73.9% in dogs without special formulation. In a HER2-expressing NCI-N87 human gastric cancer xenograft mouse model, chronic administration of TAS-116 is tolerable, with the average weight loss in mice not exceeding 10% during the treatment period[1].

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: HCT116 cells
  • Concentrations: 0.3, 1 and 3 μM
  • Incubation Time: 8 hours
  • Method:

    HCT116 cells are treated with TAS-116 or 17-AAG for 8 hours. Western blotting is performed by using 10 μg of cell lysate.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Six-week-old male BALB/c nude mice subcutaneously implanted with cancer cells
  • Dosages: 3.6 to 14.0 mg/kg/day
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

Chemical Information

Molecular Weight 454.53
Formula

C25H26N8O

CAS No. 1260533-36-5
Storage powder
in solvent
Synonyms N/A
Smiles CCC1=C(C=CC(=C1)C(N)=O)[N]2N=C(C(C)C)C3=C(C=CN=C23)[N]4C=NC(=C4)C5=C[N](C)N=C5

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID