Art. -Nr.: HY-50683

JNJ-38877605

Name: JNJ-38877605
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SKU: HY-50683
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6 Cited Publications

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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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Reinheit: 99.95%
CAS. Nr.: 943540-75-8
Formel: C₁₉H₁₃F₂N₇
Molecular Weight:377.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JNJ-38877605 Chemical Structure

CAS. Nr.: 943540-75-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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	8.4 nM Compound: 53	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	[PMID: 37262349]
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	18.6 nM Compound: 53	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	[PMID: 37262349]
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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 943540-75-8
Appearance Solid
Molecular Weight 377.35
Formel C₁₉H₁₃F₂N₇
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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
Acta Pharm Sin B

2026 Mar 2.
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.
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
Technical University of Dresden

2025.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6501 mL

13.2503 mL

26.5006 mL

5 mM

0.5300 mL

2.6501 mL

5.3001 mL

10 mM

0.2650 mL

1.3250 mL

2.6501 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Perera T, et al. JNJ-38877605: a selective Met kinase inhibitor inducing regression of Met-driven tumor models. Presented at the 99th AACR Annual Meeting; 2008 Apr 12-16

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

JNJ-38877605

6 Cited Publications

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JNJ-38877605

Publications Citing Use of MedChemExpress (MCE) JNJ-38877605