JNJ-38877605

For research use only.

Catalog No.S1114

28 publications

JNJ-38877605 Chemical Structure

Molecular Weight(MW): 377.35

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.

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Selleck's JNJ-38877605 has been cited by 28 publications

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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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human EBC1 cells Ml3yVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn;oO|IhcA>? MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWEQ{GgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUmuOUBvVQ>? MmHrNlYxODV3MkO=
human MKN45 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 M1;wRlczKGh? MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2NTkS1JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2xNE46KG6P MYOyOlAxPTV{Mx?=
human SNU5 cells NYn3UVNYWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWC3NkBp MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQVUWgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUG1Mlghdk1? NGPOb4YzPjByNUWyNy=>
mouse BAF3/TPR-Met cells  NIDBWI5Rem:uaX\ldoF1cW:wIHHzd4F6 M2XIdlczKGh? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDRkOvWHBTNU2ndDDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MUeuOkBvVQ>? NHTSOJczPjByNUWyNy=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-MET / HSP27 / p-HSP27 / HSP70 / HSP90 ; 

PubMed: 24903273     


Western blot analysis of phospho-MET, HSP27, phospho-HSP27, HSP70, and HSP90 in GTL-16 cells on treatment with JNJ-38877605; the drug was added at the doses and times shown.

p-EGFR / EGFR / p-FAK / FAK / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 31695034     


Western blotting of cMET and its downstream targets in SUM159 cells after treatment with various concentrations of JNJ38877605 for 24 h. The antibodies used for the western blotting analysis were listed in the panels

24903273 31695034
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]

Protocol

Animal Research:[3]
- Collapse
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 37 mg/mL (98.05 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 377.35
Formula

C19H13F2N7

CAS No. 943540-75-8
Storage powder
in solvent
Synonyms N/A
Smiles C[N]1C=C(C=N1)C2=N[N]3C(=NN=C3C(F)(F)C4=CC5=C(C=C4)N=CC=C5)C=C2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID