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

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

Cat. No.: HY-16069A Purity: 98.82%
COA
SDS
Handling Instructions Technical Support

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

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

CAS No. : 1429755-56-5

Size Price 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
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 15 publication(s) in Google Scholar

Other Forms of Tucatinib hemiethanolate:

Tucatinib hemiethanolate Related Antibodies

Top Publications Citing Use of Products

    Tucatinib hemiethanolate 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 hemiethanolate 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 hemiethanolate 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 hemiethanolate 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 hemiethanolate 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.

    View All EGFR Isoform Specific Products:

    View All Isoforms
    EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    IC50: 8 nM (HER2)[1]
    In Vitro

    Tucatinib hemiethanolate 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 hemiethanolate Related Antibodies
    In Vivo

    Tucatinib hemiethanolate (ONT-380 hemiethanolate, 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) hemiethanolate 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.
    Molecular Weight

    503.57

    Formula

    C26H24N8O2.1/2C2H6O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5.CCO
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (248.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9858 mL 9.9291 mL 19.8582 mL
    5 mM 0.3972 mL 1.9858 mL 3.9716 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (4.13 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.08 mg/mL.

      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 (4.13 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.08 mg/mL.

      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.
    Purity & Documentation
    References

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9858 mL 9.9291 mL 19.8582 mL 49.6455 mL
    5 mM 0.3972 mL 1.9858 mL 3.9716 mL 9.9291 mL
    10 mM 0.1986 mL 0.9929 mL 1.9858 mL 4.9646 mL
    15 mM 0.1324 mL 0.6619 mL 1.3239 mL 3.3097 mL
    20 mM 0.0993 mL 0.4965 mL 0.9929 mL 2.4823 mL
    25 mM 0.0794 mL 0.3972 mL 0.7943 mL 1.9858 mL
    30 mM 0.0662 mL 0.3310 mL 0.6619 mL 1.6549 mL
    40 mM 0.0496 mL 0.2482 mL 0.4965 mL 1.2411 mL
    50 mM 0.0397 mL 0.1986 mL 0.3972 mL 0.9929 mL
    60 mM 0.0331 mL 0.1655 mL 0.3310 mL 0.8274 mL
    80 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6206 mL
    100 mM 0.0199 mL 0.0993 mL 0.1986 mL 0.4965 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Tucatinib hemiethanolate 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:

    Tucatinib hemiethanolate1429755-56-5Irbinitinib hemiethanolate ARRY-380 hemiethanolate ONT-380 hemiethanolateEGFREpidermal growth factor receptorErbB-1HER1SolidTumorbreastcancerErbB2Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Tucatinib hemiethanolate
    Cat. No.:
    HY-16069A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (419 KB) Français - FR (419 KB) Deutsch - DE (419 KB) Norwegian - NO (419 KB) Español - ES (419 KB) Swedish - SV (419 KB) Italian - IT (419 KB) Korean - KR (419 KB) Portuguese - PT (419 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.