Pimitespib (Synonyms: TAS-116)

Name: Pimitespib
Brand: MedChemExpress
SKU: HY-15785
Rating: 5.0 (9 reviews)

Cat. No.: HY-15785 Purity: 99.87%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

For research use only. We do not sell to patients.

CAS No. : 1260533-36-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE Pimitespib

In Vivo Efficacy Study

RT-PCR

Histological Imaging/Staining

: Pimitespib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jan 7;26(2):441.; Pimitespib (TAS-116) (1.7 mg/kg; p.o.; five times a week for 18 d) reduced the amount of white blood cells and total protein in the bronchoalveolar lavage fluid (BALF) of rabbits.

: Pimitespib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jan 7;26(2):441.; Pimitespib (TAS-116) (1.7 mg/kg; p.o.; five times a week for 18 d) significantly reduced the HCl-increased expression levels of collagen 1α2 and fibronectin in rabbit lung.

: Pimitespib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jan 7;26(2):441.; Pimitespib (TAS-116) (1.7 mg/kg; p.o.; five times a week for 18 d) treatment reduced the HCl-induced activation of HSP90 and constitutive expression of ERK in rabbit lung.

: Pimitespib purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jan 7;26(2):441.; Pimitespib (TAS-116) (1.7 mg/kg; p.o.; five times a week for 18 d) treatment resulted in a milder level of chronic lung injury, minimal fibrotic response, and conserved alveolar and septal lung structure in rabbits.

: Pimitespib purchased from MedChemExpress. Usage Cited in: JTO Clin Res Rep. 2023 Jan 24;4(3):100462.; Pimitespib (1 μM; 24 h) treatment decreased levels of EGFR and AKT, which were client proteins of HSP90, and induced a nonphosphorylated, stabilized form of Bim and cleavage of full-length PARP in Ba/F3-insSVD-C797S.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HSP Isoform Specific Products:

View All Isoforms

HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

HSP90α

34.7 nM (Ki)

HSP90β

21.3 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
SK-BR-3	IC₅₀	330 nM Compound: 16e	Growth inhibition of human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of human SK-BR-3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 30525599]

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 without inhibiting other Hsp-90 family proteins such as GRP94 in endoplasmic reticulum or TRAP-1 in mitochondria^[3].
Pimitespib (0-5 μM, 48 hours) inhibits human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cells growth^[2].
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) than 17-AAG in INA6 and NCI-H929 MM cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:	Human retinal pigment epithelial ARPE-19 cell lines and NCI-H929 MM cells
Concentration:	0-5 μM
Incubation Time:	48 hours
Result:	Inhibited NCI-H929 MM cells growth with an IC₅₀ of 0.35 μM.

Western Blot Analysis^[2]

Cell Line:	MM cell lines INA6 and NCI-H929 cells
Concentration:	0.125-1 μM
Incubation Time:	24 hours
Result:	Targeted potently HSP90 client proteins including C-Raf and MEK1/2; as well as inhibited upregulation of HSP27 and overcomes 17-AAG resistance mechanisms.

In Vivo

Pimitespib (12.0 mg/kg, p.o., 14 days) shows antitumor activity without inducing eye injury in rats. Pimitespib is distributed less in retina than in plasma in rats; consequently, Pimitespib does not produce any detectable photoreceptor injury^[1].
Pimitespib triggers enhanced in vivo anti-MM activities, both alone and in combination with PS-341 (BTZ), with a favorable safety profile. Mice treated with Pimitespib (10 mg/kg and 15 mg/kg, orally, 38 days), BTZ, or Pimitespib plus BTZ show significantly enhance growth inhibition versus the vehicle control group. Median overall survival of treated animals (Pimitespib, 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^[2].
The favorable pharmacokinetic profile of Pimitespib is reflected in its dose-dependent antitumor activity; the T/C (tumor volume of Pimitespib-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. Pimitespib is orally absorbed and has a bioavailability of almost 100% in mice, and 69.0% in rats. Pimitespib has moderate terminal elimination half-life (t_1/2=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.)). Pimitespib is more rapidly eliminated from retina (t_1/2=3.4 hours) than the other HSP90 inhibitors (t_1/2=7.1-19.1 hours)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male F344 nude rats (6 weeks old) with established NCI-H1975 xenografts (6 weeks old)^[1]
Dosage:	12.0 mg/kg
Administration:	Oral administration; daily; two weeks
Result:	Led to tumor shrinkage. Showed antitumor activity without inducing eye injury in rats and did not cause ocular toxicity at the effective dose in the NCI-H1975 rat xenograft model.

Animal Model:	CB17 SCID mice (48-54 days old) with murine xenograft model^[2]
Dosage:	10 and 15 mg/kg
Administration:	Oral administration; 5 days a week; for 28 days
Result:	Enhanced significantly growth inhibition versus the vehicle control group. The delay in tumor growth was greater in the combination-treated group compared with either monotherapy cohort.

Animal Model:	Mice, Rats, and Dogs^[1]
Dosage:	3.0 mg/kg for dogs, 4.0 mg/kg for rats, 3.6, 7.1 and 14.0 mg/kg for mice
Administration:	Oral administration; daily; 20 days
Result:	Absorbed orally and had a bioavailability of almost 100% in mice, 69.0% in rats, and 73.9% in dogs without special formulation.

Clinical Trial

Molecular Weight

454.53

Formula

C₂₅H₂₆N₈O

CAS No.

1260533-36-5

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (275.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2001 mL	11.0004 mL	22.0007 mL
5 mM	0.4400 mL	2.2001 mL	4.4001 mL
10 mM	0.2200 mL	1.1000 mL	2.2001 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (252 KB) HNMR (138 KB) RP-HPLC (226 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[3]. Utsugi T. New challenges and inspired answers for anticancer drug discovery and development. Jpn J Clin Oncol. 2013 Oct;43(10):945-53. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2001 mL	11.0004 mL	22.0007 mL	55.0019 mL
	5 mM	0.4400 mL	2.2001 mL	4.4001 mL	11.0004 mL
	10 mM	0.2200 mL	1.1000 mL	2.2001 mL	5.5002 mL
	15 mM	0.1467 mL	0.7334 mL	1.4667 mL	3.6668 mL
	20 mM	0.1100 mL	0.5500 mL	1.1000 mL	2.7501 mL
	25 mM	0.0880 mL	0.4400 mL	0.8800 mL	2.2001 mL
	30 mM	0.0733 mL	0.3667 mL	0.7334 mL	1.8334 mL
	40 mM	0.0550 mL	0.2750 mL	0.5500 mL	1.3750 mL
	50 mM	0.0440 mL	0.2200 mL	0.4400 mL	1.1000 mL
	60 mM	0.0367 mL	0.1833 mL	0.3667 mL	0.9167 mL
	80 mM	0.0275 mL	0.1375 mL	0.2750 mL	0.6875 mL
	100 mM	0.0220 mL	0.1100 mL	0.2200 mL	0.5500 mL

Pimitespib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pimitespib1260533-36-5TAS-116TAS116TAS 116HSPHeat shock proteinsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Pimitespib (Synonyms: TAS-116)

Customer Review

Pimitespib Related Antibodies

9 Publications Citing Use of MCE Pimitespib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HSP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Pimitespib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Pimitespib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report