JNJ-38877605

Catalog No.S1114

For research use only.

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

CAS No. 943540-75-8

Selleck's JNJ-38877605 has been cited by 44 publications

Purity & Quality Control

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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 NV7nc|dLWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{fSSVczKGh? NEjwWoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFXCR|Eh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVkvPSCwTR?= NEDlOY8zPjByNUWyNy=>
human MKN45 cells NXLlZ2w5WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlnmO|IhcA>? NWO0fXdmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNT241PSClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OTBwOTDuUS=> MmPNNlYxODV3MkO=
human SNU5 cells MoSwVJJwdGmoZYLheIlwdiCjc4PhfS=> MXS3NkBp NVTLc|Y6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUnU2KGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF0yPS56IH7N MlPKNlYxODV3MkO=
mouse BAF3/TPR-Met cells  NXfaVVVTWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVrQdGNMPzJiaB?= M165OWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViQlHGN{9VWFJvTXX0JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2xO{43KG6P MmO0NlYxODV3MkO=
Assay
Methods Test Index PMID
Western blot p-EGFR / EGFR / p-FAK / FAK / p-AKT / AKT / p-ERK / ERK ; p-MET / HSP27 / p-HSP27 / HSP70 / HSP90 31695034 24903273
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 (from reference)

Animal Research:[3]
  • 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.

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

Chemical Information

Molecular Weight 377.35
Formula

C19H13F2N7

CAS No. 943540-75-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00651365 Terminated Drug: JNJ-38877605 Neoplasms Johnson & Johnson Pharmaceutical Research & Development L.L.C.|Ortho Biotech Inc. February 2008 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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