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

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  • 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 [1]
IC50 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]
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.
Formulation JNJ-38877605 is dissolved in PBS.
Dosages ≤40 mg/kg/day
Administration Administered via p.o.
Solubility 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Perera T, et al. Presented at the 99th AACR Annual Meeting; 2008 Apr 12-16; San Diego (CA): Abst

[2] De Bacco F, et al. J Natl Cancer Inst. 2011 Apr, 103(8), 645-661.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00651365 Terminated Neoplasms Johnson & Johnson Pharmaceutical Research & Development,  ...more Johnson & Johnson Pharmaceutical Research & Development, L.L.C.|Ortho Biotech, Inc. February 2008 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
Synonyms
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 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 PLoS One 2012 7, e44937. JNJ-38877605 purchased from Selleck
Method Western Blot
Cell Lines RPE50 cells
Concentrations
Incubation Time 0.5 h
Results

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Rating
Source PLoS One 2012 7, 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.

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Rating
Source PLoS One 2012 7, 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 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 (8)

Tech Support & FAQs

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