2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Tucatinib

Tucatinib  (Synonyms: Irbinitinib; ARRY-380; ONT-380)

製品番号: HY-16069 純度: 99.33%
COA 取扱説明書 Technical Support

Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

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CAS 番号 : 937263-43-9

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 61 在庫あり
Solution
10 mM * 1 mL in DMSO USD 61 在庫あり
Solid
5 mg $58 在庫あり
10 mg $90 在庫あり
25 mg $166 在庫あり
50 mg $250 在庫あり
100 mg $450 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 15 publication(s) in Google Scholar

Other Forms of Tucatinib:

Tucatinib 関連抗体

Top Publications Citing Use of Products

    Tucatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 23;16(1):7870.  [Abstract]

    Heatmap of the inhibitory effect of Ceritinib, Pyrotinib and Tucatinib on 76 tyrosine kinases at a concentration of 1 μM.

    Tucatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Aug 23;16(1):7870.  [Abstract]

    Dose–response curves of primary SFT cells treated with ceritinib, pyrotinib, tucatinib (0-10 μM, 72 h), E260, and DS21360717 (biological replicates n = 3).

    Tucatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Apr 1;12(4):1022-1045.  [Abstract]

    HER2+ breast cancer cell lines were treated with 1.2 μM Tucatinib (0-49 days), counted at the indicated times, and the percentage of the initial cell number was determined.

    Tucatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Apr 1;12(4):1022-1045.  [Abstract]

    GSEA shows enrichment of “Hallmark Epithelial Mesenchymal Transition” genes in mesenchymal-like DTPs (top) and “Hallmark Estrogen Responses Early” in luminal-like DTPs (bottom) evoked by Tucatinib.

    Tucatinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2022 Apr 1;12(4):1022-1045.  [Abstract]

    Heatmaps show supervised clustering of Parental, Lapatinib-DTPs and Tucatinib-DTPs with mesenchymal-DTP DEGs (left) or luminal DTP DEGs (right). Scale represents the z-score.

    EGFR 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
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.

    IC50 & Target

    HER2

     

    体外実験

    Tucatinib has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].
    Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the EGFR overexpressing cell lines, it weakly inhibits phosphorylation and proliferation, demonstrating that Tucatinib may have potential to block HER2 signaling without causing the toxicities of EGFR inhibition[1].

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

    Tucatinib 関連抗体
    体内実験

    Tucatinib (ONT-380, 200 mg/kg/d) shows a survival benefit when each drug is dosed at the maximum-tolerated dose[1].
    Tucatinib and its active metabolite causes a significant reduction in brain pErbB2 (80%)[2].
    Tucatinib (ARRY-380) demonstrates significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size) at the higher dose level in 9/12 animals. Tucatinib (50 mg/kg/d) in combination with trastuzumab shows a 98% TGI with complete regressions in 9/12 animals and two partial regressions[3].

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

    Animal Model: Female nude mice[3].
    Dosage: 200 mg/kg/d.
    Administration: PO, daily.
    Result: Exhibited anti-tumor activity and benefited survival.
    臨床実験
    分子量

    480.52

    分子式

    C26H24N8O2
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5
    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 : 41.67 mg/mL (86.72 mM; ultrasonic and warming and heat to 60°C; 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 2.0811 mL 10.4054 mL 20.8108 mL
    5 mM 0.4162 mL 2.0811 mL 4.1622 mL
    10 mM 0.2081 mL 1.0405 mL 2.0811 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.62 mg/mL (5.45 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  30% SBE-β-CD in Saline

      Solubility: 10 mg/mL (20.81 mM); Suspension solution; Need ultrasonic

    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: 99.82%

    COA (259 KB) HNMR (303 KB) LCMS (97 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0811 mL 10.4054 mL 20.8108 mL 52.0270 mL
    5 mM 0.4162 mL 2.0811 mL 4.1622 mL 10.4054 mL
    10 mM 0.2081 mL 1.0405 mL 2.0811 mL 5.2027 mL
    15 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4685 mL
    20 mM 0.1041 mL 0.5203 mL 1.0405 mL 2.6013 mL
    25 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0811 mL
    30 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
    40 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3007 mL
    50 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
    60 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
    80 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
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    • Your name will appear on the site.

    Tucatinib Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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:

    Tucatinib937263-43-9Irbinitinib ARRY-380 ONT-380ARRY380ARRY 380ARRY-380ONT380ONT 380ONT-380EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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    製品名:
    Tucatinib
    製品番号:
    HY-16069
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