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

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

Cat. No.: HY-12678 Purity: 99.87%
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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

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10 mM * 1 mL in DMSO
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10 mg USD 99 In-stock
50 mg USD 209 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Entrectinib:

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.

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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.

    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)

    *"≥" 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
    10 mM 0.1784 mL 0.8918 mL 1.7837 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% MC  0.5% Tween-80

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

    • 2.

      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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (3.71 mM); Suspended solution; Need ultrasonic

    • 6.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.87%

    References
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    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.

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