2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. JNJ-38877605

JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach.

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

JNJ-38877605 Chemical Structure

JNJ-38877605 Chemical Structure

CAS No. : 943540-75-8

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of JNJ-38877605:

JNJ-38877605 Related Antibodies

Top Publications Citing Use of Products

    JNJ-38877605 purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2020 Jun 10;11(1):229.  [Abstract]

    After disrupting c-Met phosphorylation by JNJ-38877605, activation of the Akt pathway and expression of Survivin, CDK1, and Cyclin B1 decreased compared to that of cells treated with HGF and DMSO, while cleaved Caspase-3 increased, indicating reduced proliferation and enhanced apoptosis.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    JNJ-38877605 is an orally active ATP-competitive inhibitor of c-Met with an IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases[1][2]. JNJ-38877605 inhibits c-Met phosphorylation and regulates lipid accumulation. JNJ-38877605 can be used for tumor and metabolic disease reseach[3][4][5].

    IC50 & Target[1]

    c-Met

    4 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    BaF3 IC50
    17.6 nM
    Compound: 2, JNJ38877605
    Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
    Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
    		[PMID: 26005523]
    BaF3 IC50
    8.6 nM
    Compound: JNJ38877605
    Inhibition of TPR-MET in mouse BAF3 cells assessed as reduction in cell proliferation after 72 hrs by SRB or MTT assay
    Inhibition of TPR-MET in mouse BAF3 cells assessed as reduction in cell proliferation after 72 hrs by SRB or MTT assay
    		[PMID: 27061987]
    EBC-1 IC50
    9.5 nM
    Compound: 2, JNJ38877605
    Antiproliferative activity against human EBC1 cells after 72 hrs
    Antiproliferative activity against human EBC1 cells after 72 hrs
    		[PMID: 26005523]
    MKN-45 IC50
    10.9 nM
    Compound: 2, JNJ38877605
    Antiproliferative activity against human MKN45 cells after 72 hrs
    Antiproliferative activity against human MKN45 cells after 72 hrs
    		[PMID: 26005523]
    MKN-45 IC50
    9.5 nM
    Compound: JNJ38877605
    Inhibition of c-Met in human MKN45 cells assessed as reduction in cell proliferation after 72 hrs by SRB or MTT assay
    Inhibition of c-Met in human MKN45 cells assessed as reduction in cell proliferation after 72 hrs by SRB or MTT assay
    		[PMID: 27061987]
    SNU-5 IC50
    15.8 nM
    Compound: 2, JNJ38877605
    Antiproliferative activity against human SNU5 cells after 72 hrs
    Antiproliferative activity against human SNU5 cells after 72 hrs
    		[PMID: 26005523]
    In Vitro

    JNJ-38877605 (0.5 μΜ, 24 h) inhibits CPNE1 (HY-P70097)-induced activation of the MET signaling pathway in A549 cells[4].
    JNJ-38877605 (JNJ) (5, 10, 20 μΜ, 2, 5, 8 days) inhibits c-Met phosphorylation and results in less lipid accumulation and triglyceride (TG) content with no cytotoxicity in 3T3-L1 cells[5].

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

    JNJ-38877605 Related Antibodies

    Western Blot Analysis[4]

    Cell Line: A549 cells
    Concentration: 0.5 μΜ
    Incubation Time: 24 h
    Result: Inhibited CPNE1 (HY-P70097)-induced MET phosphorylation and activation of the MET signaling pathway.

    Western Blot Analysis[5]

    Cell Line: 3T3-L1 cells
    Concentration: 5,10,20 μΜ
    Incubation Time: 2, 5, 8 day
    Result: Strongly inhibited c-Met phosphorylation without altering its total expression resulted in less lipid accumulation and triglyceride (TG) content with no cytotoxicity.
    Reduced the expression of adipogenic regulators, including CCAAT/enhancer-binding protein-α (C/EBP-α), peroxisome proliferator-activated receptor-γ (PPAR-γ), fatty acid synthase (FAS), acetyl CoA carboxylase (ACC), and perilipin A.
    Increased cAMP-activated protein kinase (AMPK) and liver kinase B-1 (LKB-1) phosphorylation but decreased ATP levels.
    In Vivo

    JNJ-38877605 (50 mg/kg, p.o., once daily for 13 days) counteractes radiation-induced invasiveness, promotes apoptosis in tumor xenografts[2].
    JNJ-38877605 (40 mg/kg, p.o., once daily for 3 days) decreases in plasma concentration of IL8, GROa, uPAR Met-addicted GTL16 xenografts mice model[3].

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

    Animal Model: U251 human glioma cells and MDA-MB-231 human breast cancer cells transplanted tumor xenografts[2]
    Dosage: 50 mg/kg
    Administration: Oral gavage (p.o.) once daily for 13 days
    Result: Counteracted radiation-induced invasiveness, promoted apoptosis.
    Animal Model: Met-addicted GTL16 xenografts mice model[3]
    Dosage: 40 mg/kg
    Administration: Oral gavage (p.o.) once daily for 3 days
    Result: Decreased in the plasma levels of human IL-8 (from 0.150 to 0.050 ng/ml) and GROa (from 0.080 to 0.030 ng/ml). Diminished The blood concentration of uPAR also by more than 50% . Inhibited Met-addicted xenografts induced consistent changes in plasma concentration of IL8, GROa, uPAR and IL-6.
    Clinical Trial
    Molecular Weight

    377.35

    Formula

    C19H13F2N7
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    FC(F)(C1=NN=C2C=CC(C3=CN(C)N=C3)=NN21)C4=CC5=C(N=CC=C5)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 : 25 mg/mL (66.25 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 2.6501 mL 13.2503 mL 26.5006 mL
    5 mM 0.5300 mL 2.6501 mL 5.3001 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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    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.63 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
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    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: 99.95%

    SDS (393 KB)

    COA (260 KB) HNMR (226 KB) LCMS (121 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 2.6501 mL 13.2503 mL 26.5006 mL 66.2515 mL
    5 mM 0.5300 mL 2.6501 mL 5.3001 mL 13.2503 mL
    10 mM 0.2650 mL 1.3250 mL 2.6501 mL 6.6251 mL
    15 mM 0.1767 mL 0.8834 mL 1.7667 mL 4.4168 mL
    20 mM 0.1325 mL 0.6625 mL 1.3250 mL 3.3126 mL
    25 mM 0.1060 mL 0.5300 mL 1.0600 mL 2.6501 mL
    30 mM 0.0883 mL 0.4417 mL 0.8834 mL 2.2084 mL
    40 mM 0.0663 mL 0.3313 mL 0.6625 mL 1.6563 mL
    50 mM 0.0530 mL 0.2650 mL 0.5300 mL 1.3250 mL
    60 mM 0.0442 mL 0.2208 mL 0.4417 mL 1.1042 mL
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    JNJ-38877605 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:

    JNJ-38877605943540-75-8JNJ38877605JNJ 38877605c-Met/HGFRc-Metlipid accumulationAMPK3T3-L1A549 cellstumor xenograftsInhibitorinhibitorinhibit

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