Pimitespib (TAS-116)

Catalog No.S7716 Batch:S771601

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Technical Data

Formula

C25H26N8O
Molecular Weight 454.53 CAS No. 1260533-36-5
Solubility (25°C)* In vitro DMSO 91 mg/mL (200.2 mM)
Ethanol 11 mg/mL (24.2 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Pimitespib (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].
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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • 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

Selleck's Pimitespib (TAS-116) has been cited by 2 publications

Syringaresinol inhibits cardiorenal fibrosis through HSP90 in a cardiorenal syndrome type 2 [ Hum Exp Toxicol, 2023, 42:9603271231165678] PubMed: 36960691
Single-cell dissection of the multiomic landscape of high-grade serous ovarian cancer [ Cancer Res, 2022, CAN-21-3819] PubMed: 35969151

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.