2. Protein Tyrosine Kinase/RTK Neuronal Signaling Autophagy
  3. ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy
  4. Entrectinib

Entrectinib  (Synonyms: NMS-E628; RXDX-101)

Cat. No.: HY-12678 Purity: 99.79%
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Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.

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

Entrectinib Chemical Structure

Entrectinib Chemical Structure

CAS No. : 1108743-60-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 81 In-stock
Solution
10 mM * 1 mL in DMSO USD 81 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 66 In-stock
10 mg USD 99 In-stock
50 mg USD 209 In-stock
100 mg USD 363 In-stock
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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of Entrectinib:

Entrectinib Related Antibodies

Top Publications Citing Use of Products

    Entrectinib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107994.  [Abstract]

    Immunoblot analysis of protein expression or modification in lysates of IMPETPR-NTRK1 cells treated with 10 nM Entrectinib for 0-24 h. pTRKA remained completely inhibited at 18 and 24 h, indicating that Entrectinib is still effectively inhibiting its direct target.

    Entrectinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Oct;16(10):2130-2143.  [Abstract]

    KM12 or CR20 cells are treated with increasing concentrations of Cabozantinib, Entrectinib or LOXO-101 for 3 hours. Cell lysates are immunoblotted to detect the indicated proteins.

    View All Trk Receptor Isoform Specific Products:

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    TrkA TrkB TrkC Trk

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    Description

    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice[1][2][3].

    IC50 & Target

    IC50: 1 nM (TrkA), 3 nM (TrkB), 5 nM (TrkC), 12 nM (ROS1), 7 nM (ALK)[2].
    In Vitro

    Entrectinib (100, 200, 400 nM; 24 h) alleviates TGF-β1-induced activation of mouse lung fibroblasts[1].
    Entrectinib(100, 200, 400 nM; 24 h) inhibits TGF-β1-induced epithelial to mesenchymal transition of mouse lung epithelial cells[1].
    Entrectinib (10, 50, 250 nM; 2 h) abolishes autophosphorylation of TPM3-TRKA, concomitant with complete inhibition of the phosphorylation of PLCg1, AKT, and MAPK in KM12 cells[2].
    Entrectinib (10, 50, 250 nM; 24, 48 h) induce KM12 cells cycle arrest (24 h) and apoptosis (48 h)[2].

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

    Entrectinib Related Antibodies

    Western Blot Analysis[1]

    Cell Line: Mouse lung fibroblasts cells
    Concentration: 100, 200, 400 nM
    Incubation Time: 24 h
    Result: Reduced the protein expression levels of α-SMA, collagen I and fibronectin in the TGF-β1-treated fibroblasts.

    Western Blot Analysis[1]

    Cell Line: Mouse lung epithelial cells
    Concentration: 100, 200, 400 nM
    Incubation Time: 24 h
    Result: Significantly increased the expression of the epithelial marker Ecadherin and decreased the expression of the mesenchymal markers N-cadherin and Vimentin.

    Apoptosis Analysis[2]

    Cell Line: KM12 cells
    Concentration: 10, 50, 250 nM
    Incubation Time: 24, 48 h
    Result: Induced accumulation of cells in the G1 phase of the cell cycle at 24 hours treatment, followed by apoptosis induction at 48 hours.
    In Vivo

    Entrectinib (20, 40, 60 mg/kg; i.g.; single daily for 7 days) attenuates bleomycin-induced pulmonary fibrosis in mice[1].
    Entrectinib (30, 60 mg/kg; p.o.; twice daily for 10 consecutive days) induces regression of xenograft tumors in tumor-bearing mice, including TRKA-dependent colorectal cancer KM12, ROS1-driven tumors, and several ALK-dependent models of different tissue origins, including brain-localized lung model cancer metastasis[2].

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

    Animal Model: Male C57BL/6 mice (6-8 weeks old, 20-25 g; Bleomycin-induced pulmonary fibrosis model)[1].
    Dosage: 20, 40, 60 mg/kg
    Administration: Intragastric Administration; single daily for 7 days.
    Result: Significantly improved lung function in the pulmonary fibrosis model mice.
    Clinical Trial
    Molecular Weight

    560.64

    Formula

    C31H34F2N6O2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=C(NC5CCOCC5)C=C(N6CCN(C)CC6)C=C4
    Shipping

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

    DMSO : ≥ 31 mg/mL (55.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7837 mL 8.9184 mL 17.8368 mL
    5 mM 0.3567 mL 1.7837 mL 3.5674 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.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (4.46 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:  0.5% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 5 mg/mL (8.92 mM); Suspended solution; Need ultrasonic

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

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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: 99.79%

    COA (252 KB) HNMR (281 KB) LCMS (94 KB) Elemental Analysis Report (110 KB)

    Handling Instructions (2659 KB)
    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, 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 1.7837 mL 8.9184 mL 17.8368 mL 44.5919 mL
    5 mM 0.3567 mL 1.7837 mL 3.5674 mL 8.9184 mL
    10 mM 0.1784 mL 0.8918 mL 1.7837 mL 4.4592 mL
    15 mM 0.1189 mL 0.5946 mL 1.1891 mL 2.9728 mL
    20 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
    25 mM 0.0713 mL 0.3567 mL 0.7135 mL 1.7837 mL
    30 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4864 mL
    40 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
    50 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
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    Entrectinib 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:

    Entrectinib1108743-60-7NMS-E628 RXDX-101RXDX101RXDX 101RXDX-101ROS KinaseTrk ReceptorAnaplastic lymphoma kinase (ALK)AutophagyTropomyosin related kinase receptor Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246KM12 cellscancerlung fibrosistumorfibroblasts cellsInhibitorinhibitorinhibit

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