Pimitespib

SKU: orb1307700

Description

Pimitespib (TAS-116) is a potent and selective ATP-competitive inhibitor targeting both HSP90α and HSP90β isoforms. It has demonstrated antitumor activity in preclinical models, supporting its research use in oncology for investigating HSP90's role in protein folding and cancer cell survival.

Research Area

Metabolism Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1260533-36-5
MW	454.53
Purity	99.49% (May vary between batches)
Formula	C₂₅H₂₆N₈O
SMILES	CCc1cc(ccc1-n1nc(C(C)C)c2c(ccnc12)-n1cnc(c1)-c1cnn(C)c1)C(N)=O
Target	HSP
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.8 mM);DMSO:50 mg/mL (110 mM)

Bioactivity

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Target IC50	HSP90 β:21.3 nM (Ki)\|HSP90 α:34.7 nM (Ki)
In Vivo	TAS-116 is orally absorbed and has a bioavailability of almost 100% in mice, and 69.0% in rats. TAS-116 has moderate terminal elimination half-life (t1/2=8.2 h, 2.5 h, 4.4 h and 2.2 h for mouse (3.6 mg/kg, p.o.), mouse (7.1 mg/kg, p.o.), mouse (14.0 mg/kg, p.o.), rat (4 mg/kg, p.o.)). TAS-116 is more rapidly eliminated from retina (t1/2=3.4 hours) than the other HSP90 inhibitors (t1/2=7.1-19.1 hours). TAS-116 is distributed less in retina than in plasma in rats; consequently, TAS-116 does not produce any detectable photoreceptor injury. TAS-116 triggers enhanced in vivo anti-MM activities, both alone and in combination with Bortezomib (BTZ), with a favorable safety profile. TAS-116 (12.0 mg/kg, p.o., 14 days) displays antitumor activity without inducing eye injury in rats. Mice treated with TAS-116 (10 mg/kg and 15 mg/kg, orally, 38 days), BTZ, or TAS-116 plus BTZ show significantly enhance growth inhibition versus the vehicle control group. Median overall survival of treated animals (TAS-116, orally, 10 mg/kg=33 days, 15 mg/kg=37 days, BTZ=36 days, and the combination=56.5 days) is significantly longer than vehicle control. The favorable pharmacokinetic profile of TAS-116 is reflected in its dose-dependent antitumor activity; the T/C (tumor volume of TAS-116-treated mice vs. vehicle-treated mice) is 47%, 21%, and 9% for doses of 3.6 mg/kg, 7.1 mg/kg, and 14.0 mg/kg, respectively . Read more...
In Vitro	Pimitespib binds not only to the conventional-binding pockets as existing Hsp-90 inhibitors but also to a novel-binding pocket. Such a unique binding mode makes Pimitespib highly specific for Hsp-90α/β. Pimitespib (0-5 μM, 48 hours) inhibits human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cell growth. Compared 17-AAG in INA6 and NCI-H929 MM cells, more significant degradation of p-C-Raf and p-MEK1/2, HSP90 client proteins, and key RAS/RAF/MEK pathway regulators, is triggered by Pimitespib (0.125-1 μM, 24 hours) . Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Heat shock proteins, Inhibitor, HSP, HSP90α, HSP90β, inhibit, Pimitespib, TAS 116, TAS116, TAS-116

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Compound Identifiers

PubChem CID

67501411 ↗

Key Properties

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No computed properties available.

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Pimitespib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

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Protocol Information

Pimitespib (orb1307700)

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