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.

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JNJ-38877605 Chemical Structure

JNJ-38877605 Chemical Structure
Molecular Weight: 377.35

Validation & Quality Control

Customer Reviews(5)

Quality Control & MSDS

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Product Information

  • Compare c-Met Inhibitors
    Compare c-Met Inhibitors
  • Research Area

Product Description

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
IC50 4 nM [1]
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]
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]
Features

Protocol(Only for Reference)

Animal Study: [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 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00651365 Terminated Neoplasms Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|Ortho Biotech, Inc. 2008-02 Phase 1

Chemical Information

Download JNJ-38877605 SDF
Molecular Weight (MW) 377.35
Formula

C19H13F2N7

CAS No. 943540-75-8
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 37 mg/mL (98 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 6-(difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl)quinoline

Research Area

Customer Reviews (5)


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Rating
Source PLOS one, 2012. 7(9), e44937. JNJ-38877605 purchased from Selleck
Method Western Blot
Cell Lines RPE50 cells
Concentrations
Incubation Time 0.5 h
Results

Click to enlarge
Rating
Source PLOS one, 2012. 7(9), e44937. JNJ-38877605 purchased from Selleck
Method Wound healing assay
Cell Lines RPE50 and ARPE19 cells
Concentrations
Incubation Time 18 h
Results As positive controls, JNJ38877605 and AG1478, theinhibitors of c-met (the receptor of HGF) and EGFR (the receptorof both EGF and HB-EGF) abolished migration of both types of RPE cells induced by HGF and EGF, respectively.

Click to enlarge
Rating
Source PLoS One, 2012, 7(9), e44937.. JNJ-38877605 purchased from Selleck
Method Western blot
Cell Lines RPE50 cells
Concentrations 50 nM
Incubation Time 0.5 h
Results HGF-induced phosphorylation of ERK at 0.5 h can be reduced by BIS, PD98059 and JNJ38877605 by 70, 58 and 77%Respectively.

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Rating
Source PLoS Biol 2011 9, e1001162 . JNJ-38877605 purchased from Selleck
Method qRT-PCR, Immunofluorescence
Cell Lines RETAAD tumor cells, NBT-II cells, PMN-MDSCs
Concentrations
Incubation Time 24 h
Results We found that JNJ-38877605 and other inhibitors of the corresponding receptors blocked PMN-MDSC mediated induction of EMT. The fact that EGF inhibitors reduced EMT induction while PMN-MDSC purified from RETAAD tumors did not produce EGF may suggest that PMN-MDSC stimulate EGF production by the cancer cells.

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Rating
Source Dr. Zhang of Tianjin Medical University. JNJ-38877605 purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-1000 nM
Incubation Time 3 h
Results JNJ-38877605 treatment resulted in a reduction of c-Met phosphorylation in Breast cancer cells.

Product Citations (6)

Tech Support & FAQs

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.

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  • Crizotinib (PF-02341066)

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  • BMS-777607

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  • 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.

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