Home Cytoskeletal Signaling HSP (HSP90) inhibitor Pimitespib (TAS-116) For research use only.

Pimitespib (TAS-116)

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).

Pimitespib (TAS-116) Chemical Structure

Pimitespib (TAS-116) Chemical Structure

CAS No. 1260533-36-5

Purity & Quality Control

Batch: S771601 DMSO]91 mg/mL]false]Ethanol]11 mg/mL]false]Water]Insoluble]false Purity: 99.32%
99.32

Pimitespib (TAS-116) Related Products

Signaling Pathway

HSP (HSP90) Signaling Pathways

HSP (HSP90) Signaling Pathway

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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-B-Raf / B-raf / p-C-Raf / C-Raf / p-MEK / MEK / p-ERK / ERK / p-AKT / AKT / PARP 26630652
Growth inhibition assay Cell viability 26630652
In Vivo
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].
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05655598 Recruiting
Advanced Breast Cancer|Treatment-Refractory Solid Tumors|Retinoblastoma Deficiency|SCLC|Soft Tissue Sarcoma|Endometrial Cancer|Bladder Cancer
Brown University
 September 12 2023 Phase 1
NCT02965885 Completed
Advanced Solid Tumors
Taiho Oncology Inc.
 July 10 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 454.53 Formula

C25H26N8O
CAS No. 1260533-36-5 SDF --
Smiles CCC1=C(C=CC(=C1)C(=O)N)N2C3=NC=CC(=C3C(=N2)C(C)C)N4C=C(N=C4)C5=CN(N=C5)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (200.2 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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.

Handling Instructions

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