Home Protein Tyrosine Kinase c-Met inhibitor JNJ-38877605 For research use only.

JNJ-38877605

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 Chemical Structure

JNJ-38877605 Chemical Structure

CAS No. 943540-75-8

Purity & Quality Control

JNJ-38877605 Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Cell Data

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 26005523
human MKN45 cells Proliferation assay 72 h Antiproliferative activity against human MKN45 cells after 72 hrs, IC50=10.9 nM 26005523
human SNU5 cells Proliferation assay 72 h Antiproliferative activity against human SNU5 cells after 72 hrs, IC50=15.8 nM 26005523
mouse BAF3/TPR-Met cells  Proliferation assay 72 h Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs, IC50=17.6 nM 26005523
Click to View More Cell Line Experimental Data

Biological Activity

Description 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.
Targets
c-Met [1]
4 nM
In vitro
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, JNJ-38877605 (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 JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. [3]
Experimental Result Images 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 24903273
In Vivo
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]
Animal Research Animal Models GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
Dosages ≤40 mg/kg/day
Administration Administered via p.o.
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

Chemical Information & Solubility

Molecular Weight 377.35 Formula

C19H13F2N7
CAS No. 943540-75-8 SDF Download JNJ-38877605 SDF
Smiles CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2
Storage (From the date of receipt)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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