Home Protein Tyrosine Kinase c-Met inhibitor JNJ-38877605

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JNJ-38877605 c-Met inhibitor

Cat.No.S1114

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1.
JNJ-38877605 c-Met inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 377.35

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Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human EBC1 cells Proliferation assay 72 h Antiproliferative activity against human EBC1 cells after 72 hrs, IC50=9.5 nM
human MKN45 cells Proliferation assay 72 h Antiproliferative activity against human MKN45 cells after 72 hrs, IC50=10.9 nM
human SNU5 cells Proliferation assay 72 h Antiproliferative activity against human SNU5 cells after 72 hrs, IC50=15.8 nM
mouse BAF3/TPR-Met cells  Proliferation assay 72 h Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs, IC50=17.6 nM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 377.35 Formula

C19H13F2N7

 Storage (From the date of receipt)
CAS No. 943540-75-8 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2

Solubility

In vitro
Batch:

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
c-Met [1]
4 nM
In vitro
JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. [1] In EBC1, GTL16, NCI-H1993, and MKN45 cells, this compound (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. [2] A recent study shows that this chemical is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. [3]
In vivo
In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally with 40 mg/kg/day for 72 hours, results in a statistically significant decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose. [3]
References

Applications

Methods Biomarkers Images PMID
Western blot p-MET / HSP27 / p-HSP27 / HSP70 / HSP90 p-EGFR / EGFR / p-FAK / FAK / p-AKT / AKT / p-ERK / ERK S1114-WB1 24903273

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00651365 Terminated
Neoplasms
Johnson & Johnson Pharmaceutical Research & Development L.L.C.|Ortho Biotech Inc.
 February 2008 Phase 1

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