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JNJ-38877605

Cat. No. M1793
JNJ-38877605 Structure
Synonym:

JNJ38877605

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 480 In stock
100mg USD 820 In stock
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Quality Control
Biological Activity

JNJ-38877605 is a small-molecule, ATP-competitive inhibitor of the catalytic activity of c-Met. JNJ-38877605 showed f600-fold selectivity for c-Met compared with a panel of f250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In addition, JNJ-38877605 induces regression of U87-MG xenografts in vivo.

Protocol
Cell Experiment
Cell lines S114, GTL-16, NCI-H441, or BxPC-3 cells
Preparation method Cell Proliferation Assays. S114, GTL-16, NCI-H441, or BxPC-3 cells were seeded in 96-well plates at 9000 cells/well in medium with 10% FBS. After incubation for 48 h in low serum (0.5% FBS, S114; 0.1% FBS, GTL-16, NCI-H441, and BxPC-3), cells were treated with different concentrations of PHA-665752 for 18 h at 37°C. HGF (50 ng/ml) was added for 18 h before BrdUrd for studies involving GTL-16, H441, and BxPC-3. After incubation with BrdUrd labeling reagent for 1 h (Sigma Biochemicals, St. Louis, MO), cells were fixed and BrdUrd incorporation into newly synthesized DNA was assessed using anti-BrdUrd peroxidase-conjugated antibody followed by colorimetric determination at 630 nm.
Concentrations 0~1.25µM
Incubation time 18 h
Animal Experiment
Animal models Female athymic mice bearing S114 or GTL-16 tumor xenografts
Formulation L-lactate (pH 4.8) and 10% polyethylene glycol
Dosages 25 mg/kg a single i.v. dose
Administration via bolus i.v. tail vein injection
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 377.35
Formula C19H13F2N7
CAS Number 943540-75-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer.
De Bacco F, et al. J Natl Cancer Inst. 2011 Apr 20;103(8):645-61. PMID: 21464397.

Genetic and expression analysis of MET, MACC1, and HGF in metastatic colorectal cancer: response to met inhibition in patient xenografts and pathologic correlations.
Galimi F, et al. Clin Cancer Res. 2011 May 15;17(10):3146-56. PMID: 21447729.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JNJ-38877605, JNJ38877605 supplier, c-Met, inhibitors

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