Product Details
| Product Name:
Pimitespib |
CAS No.:
1260533-36-5 |
| Purity:
99.49% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Pimitespib |
| Description | Pimitespib (TAS-116) is an ATP-competitive and highly specific HSP90α/HSP90β inhibitor with inhibition constants (Kis) of 34.7 nM and 21.3 nM, respectively. |
| 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) [2][3]. |
| 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 [1][2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 125 mg/mL (275.01 mM), Sonication is recommended.
|
| Keywords | TAS116 | TAS 116 | Pimitespib | Inhibitor | inhibit | HSP | Heat shock proteins |
| Inhibitors Related | Ethoxyquin | SNX0723 | Tamoxifen | DN401 | SNX2112 | Ganetespib | Teprenone | Elesclomol | Rifabutin | Paeoniflorin | Palmitic acid | Tamoxifen Citrate |
| Related Compound Libraries | Exosome Compound Library | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Metabolism Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States