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Pimitespib

Name: Pimitespib
Brand: TargetMol
SKU: T16994
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16994Cas No. 1260533-36-5

Alias TAS-116

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.

Pimitespib

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Purity: 99.49%

Catalog No. T16994Alias TAS-116Cas No. 1260533-36-5

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.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$33	In Stock	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$198	-	In Stock
50 mg	$378	-	In Stock
1 mL x 10 mM (in DMSO)	$75	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Batch Information

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Purity:99.49%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

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.
Targets&IC50	HSP90 β:21.3 nM (Ki), HSP90 α:34.7 nM (Ki)
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].
Synonyms	TAS-116

Chemical Properties

Molecular Weight	454.53
Formula	C₂₅H₂₆N₈O
Cas No.	1260533-36-5
Smiles	CCc1cc(ccc1-n1nc(C(C)C)c2c(ccnc12)-n1cnc(c1)-c1cnn(C)c1)C(N)=O
Relative Density.	1.36 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (110 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (8.8 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2001 mL	11.0004 mL	22.0007 mL	110.0037 mL
5 mM	0.4400 mL	2.2001 mL	4.4001 mL	22.0007 mL
10 mM	0.2200 mL	1.1000 mL	2.2001 mL	11.0004 mL
20 mM	0.1100 mL	0.5500 mL	1.1000 mL	5.5002 mL
50 mM	0.0440 mL	0.2200 mL	0.4400 mL	2.2001 mL
100 mM	0.0220 mL	0.1100 mL	0.2200 mL	1.1000 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc