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JNJ-38877605

JNJ-38877605
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Purity:98.27%
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JNJ-38877605

Catalog No. T6095Cas No. 943540-75-8
JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
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Pack SizePriceAvailabilityQuantity
2 mg$34In Stock
5 mg$53In Stock
10 mg$85In Stock
25 mg$153In Stock
50 mg$247In Stock
100 mg$405In Stock
1 mL x 10 mM (in DMSO)$57In Stock
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Product Introduction

Bioactivity
Description
JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
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. 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. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells.
In vivo
In mice bearing established GTL16 xenografts, JNJ-38877605 (40 mg/kg/day, p.o., total 3day) results in a statistically marked decrease in the plasma levels of human IL-8 (0.150-0.050 ng/mL) and GROα (0.080-0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose.
Animal Research
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 immuno-deficient 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.
Chemical Properties
Molecular Weight377.35
FormulaC19H13F2N7
Cas No.943540-75-8
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 6 mg/mL (15.9 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
20 mM0.1325 mL0.6625 mL1.3250 mL6.6251 mL
50 mM0.0530 mL0.2650 mL0.5300 mL2.6501 mL
100 mM0.0265 mL0.1325 mL0.2650 mL1.3250 mL

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