Pimitespib

Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94[1]. Pimitespib demonstrates less ocular toxicity[2].

Product Specifications

CAS Number

[1260533-36-5]

Product Name Alternative

TAS-116

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

HSP

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TAS-116.html

Concentration

10mM

Purity

99.15

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=C(N)C1=CC=C(N2N=C(C(C)C)C3=C(N4C=C(C5=CN(C)N=C5)N=C4)C=CN=C32)C(CC)=C1

Molecular Formula

C25H26N8O

Molecular Weight

454.53

Precautions

H302, H315, H319, H335

References & Citations

[1]Ohkubo S, et al. TAS-116, a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models. Mol Cancer Ther. 2015 Jan;14 (1) :14-22.|[2]Suzuki R, et al. Anti-tumor activities of selective HSP90α/β inhibitor, TAS-116, in combination with PS-341 in multiple myeloma. Leukemia. 2015 Feb;29 (2) :510-4.|[3]Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43 (10) :945-53.