2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. Pimitespib

Pimitespib  (Synonyms: TAS-116)

製品番号: HY-15785 純度: 99.87%
COA 取扱説明書 Technical Support

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. Pimitespib demonstrates less ocular toxicity.

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CAS 番号 : 1260533-36-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 93 在庫あり
Solution
10 mM * 1 mL in DMSO USD 93 在庫あり
Solid
5 mg $85 在庫あり
10 mg $132 在庫あり
25 mg $275 在庫あり
50 mg $460 在庫あり
100 mg $750 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Pimitespib 関連抗体

Top Publications Citing Use of Products

    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.

    HSP アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    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].

    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]
    体外実験

    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.

    Pimitespib 関連抗体

    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.
    体内実験

    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 (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.)). Pimitespib is more rapidly eliminated from retina (t1/2=3.4 hours) than the other HSP90 inhibitors (t1/2=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.
    臨床実験
    分子量

    454.53

    分子式

    C25H26N8O
    CAS 番号
    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    Mass
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    Volume
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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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.
    純度とドキュメンテーション

    純度: 99.87%

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

    取扱説明書 (2659 KB)
    参考文献

    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.

    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
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    Pimitespib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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

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    製品名:
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    製品番号:
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