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).
|Solubility (25°C)||DMSO 91 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Emi Ikebe, et al. Cancer Sci. TAS-116 (pimitespib), a heat shock protein 90 inhibitor, shows efficacy in preclinical models of adult T-cell leukemia
 Akihito Kawazoe, et al. Clin Cancer Res. TAS-116 (Pimitespib), an Oral HSP90 Inhibitor, in Combination with Nivolumab in Patients with Colorectal Cancer and Other Solid Tumors: An Open-Label, Dose-Finding, and Expansion Phase Ib Trial (EPOC1704)
 Sofia Ranta-Aho, et al. Int J Mol Sci. TAS-116, a Well-Tolerated Hsp90 Inhibitor, Prevents the Activation of the NLRP3 Inflammasome in Human Retinal Pigment Epithelial Cells
 Yurina Saito, et al. Br J Cancer. TAS-116 inhibits oncogenic KIT signalling on the Golgi in both imatinib-naïve and imatinib-resistant gastrointestinal stromal tumours
 Younghyun Lee, et al. Mol Cancer Ther. TAS-116, a Novel Hsp90 Inhibitor, Selectively Enhances Radiosensitivity of Human Cancer Cells to X-rays and Carbon Ion Radiation
|Related HSP Products|
Arimoclomol (BRX-220 free base) is a heat shock protein (HSP) co-inducer. arimoclomol protects motor neurons by enhancing Hsp expression, thereby directly affecting protein aggregation and removing misfolded and misassembled proteins through the ubiquitin-proteasome system.
DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
WAY-270444 is a Hsp90 inhibitor/ inhibits histidine kinases C. crescentus CckA
VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.