JNJ-38877605
Based on 6 publication(s) in Google Scholar
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.
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- Pureté: 99.95%
- CAS No.: 943540-75-8
- Formule: C19H13F2N7
- Masse moléculaire:377.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) JNJ-38877605
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Activité biologique
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c-Met 4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
17.6 nM
Compound: 2, JNJ38877605
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Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs
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[PMID: 26005523] |
| BaF3 | IC50 |
8.6 nM
Compound: JNJ38877605
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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
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[PMID: 27061987] |
| EBC-1 | IC50 |
8.4 nM
Compound: 53
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Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth
Antiproliferative activity against human EBC-1 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| EBC-1 | IC50 |
9.5 nM
Compound: 2, JNJ38877605
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Antiproliferative activity against human EBC1 cells after 72 hrs
Antiproliferative activity against human EBC1 cells after 72 hrs
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[PMID: 26005523] |
| MKN-45 | IC50 |
10.9 nM
Compound: 2, JNJ38877605
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Antiproliferative activity against human MKN45 cells after 72 hrs
Antiproliferative activity against human MKN45 cells after 72 hrs
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[PMID: 26005523] |
| MKN-45 | IC50 |
18.6 nM
Compound: 53
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Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth
Antiproliferative activity against human MKN-45 cells assessed as inhibition of cell growth
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[PMID: 37262349] |
| MKN-45 | IC50 |
9.5 nM
Compound: JNJ38877605
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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
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[PMID: 27061987] |
| SNU-5 | IC50 |
15.8 nM
Compound: 2, JNJ38877605
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Antiproliferative activity against human SNU5 cells after 72 hrs
Antiproliferative activity against human SNU5 cells after 72 hrs
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[PMID: 26005523] |
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.
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Cell Line:A549 cells
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Concentration:0.5 μΜ
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Incubation Time:24 h
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Result:Inhibited CPNE1 (HY-P70097)-induced MET phosphorylation and activation of the MET signaling pathway.
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Cell Line:3T3-L1 cells
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Concentration:5,10,20 μΜ
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Incubation Time:2, 5, 8 day
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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.
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.
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Animal Model:U251 human glioma cells and MDA-MB-231 human breast cancer cells transplanted tumor xenografts[2]
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Dosage:50 mg/kg
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Administration:Oral gavage (p.o.) once daily for 13 days
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Result:Counteracted radiation-induced invasiveness, promoted apoptosis.
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Animal Model:Met-addicted GTL16 xenografts mice model[3]
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Dosage:40 mg/kg
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Administration:Oral gavage (p.o.) once daily for 3 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 943540-75-8
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Appearance Solid
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Masse moléculaire 377.35
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Formule C19H13F2N7
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Color Off-white to light yellow
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SMILES
FC(F)(C1=NN=C2C=CC(C3=CN(C)N=C3)=NN21)C4=CC5=C(N=CC=C5)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
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Stem Cell Res Ther
Pulp stem cells with hepatocyte growth factor overexpression exhibit dual effects in rheumatoid arthritis. [Abstract]2020 Jun 10;11(1):229. PMID: 32522231
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.
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Biochem Biophys Res Commun
FAXC depletion contributes to tumor progression via the c-MET pathway in renal cell carcinoma. [Abstract]2025 Sep 8:778:152388. PMID: 40706244 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[2]. De Bacco F, et al. Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer. J Natl Cancer Inst. 2011 Apr, 103(8), 645-661. [Content Brief]
[3]. Torti D, et al. A preclinical algorithm of soluble surrogate biomarkers that correlate with therapeutic inhibition of the MET oncogene in gastric tumors. Int J Cancer. 2012, 130(6), 1357-1366. [Content Brief]
[4]. Wang A, et.al. CPNE1 promotes non-small cell lung cancer progression by interacting with RACK1 via the MET signaling pathway. Cell Commun Signal. 2022 Jan 31;20(1):16. [Content Brief]
[5]. Park YK, et.al. The Receptor Tyrosine Kinase c-Met Promotes Lipid Accumulation in 3T3-L1 Adipocytes. Int J Mol Sci. 2023 Apr 29;24(9):8086. [Content Brief]
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 |
JNJ-38877605 Related Classifications
HY-50683 Related Classifications
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