JNJ-38877605

Catalog No.S1114

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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In DMSO USD 220 In stock
USD 70 In stock
USD 150 In stock
USD 270 In stock
USD 770 In stock
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6 Customer Reviews

  • Inducers of EMT. (A) Expression of Hgf, Egf, and Tgfb1 genes in RETAAD tumors analyzed by qRT-PCR. Hgf and Tgfb1 are preferentially expressed in PMN-MDSC, while Egf is preferentially expressed in tumor cells. Data are from four individual experiments using sorted fractions of PMNMDSC and melanoma cells. Bars represent mean 6 SD. (B) NBT-II cells (100 cells per well) were plated for 4 d to allow for colony growth and were pretreated for 24 h with inhibitors before the addition of PMN-MDSC. After co-culture with PMN-MDSCs in the presence of inhibitors, cells were fixed and stained with anti-rat desmoplakin. Green, Desmoplakin; red, H2b (nuclear stain). PD153035-EGFR inhibitor, JNJ38877605-c-met (HGFR) inhibitor, and SB525334-TGF-bR1 inhibitor. Images are representative of three independent experiments.

    PLoS Biol 2011 9, e1001162 . JNJ-38877605 purchased from Selleck.

    Western-blot analysis of MET phosphorylation and its downstream effectors AKT and ERK1/2 in two MET-dependant cell lines (MHCC97H and HCC-3) treated 4 hours with increasing doses of PHA-665752, JNJ-38877605 or tivantinib.

    Clin Cancer Res, 2017. JNJ-38877605 purchased from Selleck.

  • Growth factors induced ERK phosphorylation in RPE50 and ARPE19. (B) RPE50 cells were untreated (-), treated with 50 nM of HGF or EGF or 50 ng/ml HB-EGF coupled with DMSO or various inhibitors as indicated for 0.5 h.

    PLoS One 2012 7, e44937. JNJ-38877605 purchased from Selleck.

    (C) RPE 50 (black) and ARPE19 (gray) were untreated (-), treated with 50 nM HGF , or HGF and EGF coupled with DMSO (as solvent control) or various inhibitors as indicated. Wound healing assay were performed and relative migrations were quantitated as described in (B). JNJ=JNJ38877605.

    PLoS One 2012 7, e44937. JNJ-38877605 purchased from Selleck.

  • (B) RPE50 cells were untreated (-), treated with 50 nM of HGF or EGF or 50 ng/ml HB-EGF coupled with DMSO or various inhibitors as indicated for 0.5 h.

    PLoS One 2012 7, e44937. JNJ-38877605 purchased from Selleck.

    After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of JNJ-38877605 for 3h,followed by 15-minute stimolation of 100ng/ml EGF

     
     

     

    Dr. Zhang of Tianjin Medical University. JNJ-38877605 purchased from Selleck.

Purity & Quality Control

Choose Selective c-Met Inhibitors

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 NULmTHk4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHTTbo04OiCq MoTZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCHQlOxJINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME25MlUhdk1? NILMVoEzPjByNUWyNy=>
human MKN45 cells MmmxVJJwdGmoZYLheIlwdiCjc4PhfS=> MmftO|IhcA>? M1nyOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVvOOFUh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVExNjlibl2= MWOyOlAxPTV{Mx?=
human SNU5 cells MnrLVJJwdGmoZYLheIlwdiCjc4PhfS=> M1L1[FczKGh? NFXBUXhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPOWVUh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVE2Njhibl2= MV:yOlAxPTV{Mx?=
mouse BAF3/TPR-Met cells  MkLmVJJwdGmoZYLheIlwdiCjc4PhfS=> M3q1XVczKGh? NYW3c486SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{N1SSUj3N[ZQh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVE4NjZibl2= M4C3XlI3ODB3NUKz

... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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.
  • Formulation: JNJ-38877605 is dissolved in PBS.
  • 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 individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
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

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Clinical Trial Information

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

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.

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Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID