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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
HSP90
Available Sizes
Frequently Asked Questions
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