Molecular Formula | C19H13F2N7 |
Molar Mass | 377.35 |
Density | 1.50 |
Storage Condition | -20℃ |
Refractive Index | 1.733 |
In vitro study | JNJ-38877605 is a small molecule ATP competitive c-Met inhibitor with an IC50 of 4 nM. Furthermore, JNJ-38877605 was more than 200-fold more selective at c-Met than at more than 600 other different tyrosine and serine-threonine kinases and was also effective in inhibiting HGF-stimulated and constitutively activated c-Met phosphorylation. JNJ-38877605 at a dose of 500 nM in EBC1,GTL16,NCI-H1993, and MKN45 cells, Met and RON phosphorylation was significantly reduced, which is another key factor in invasive growth. Recent studies have shown that JNJ-38877605 acts on GTL16 cells, involving the regulated secretion of IL-8,GROa,uPAR and IL-6. JNJ-38877605 is a small molecule ATP competitive c-Met inhibitor with an IC50 of 4 nM. Furthermore, JNJ-38877605 was more than 200-fold more selective at c-Met than at more than 600 other different tyrosine and serine-threonine kinases and was also effective in inhibiting HGF-stimulated and constitutively activated c-Met phosphorylation. JNJ-38877605 at a dose of 500 nM in EBC1,GTL16,NCI-H1993, and MKN45 cells, Met and RON phosphorylation was significantly reduced, which is another key factor in invasive growth. Recent studies have shown that JNJ-38877605 acts on GTL16 cells, involving the regulated secretion of IL-8,GROa,uPAR and IL-6. |
In vivo study | Oral administration of 40 mg/kg daily for 72 hours JNJ-38877605 in mice bearing GTL16 xenografts significantly reduced plasma levels in humans by IL-8 (from 0.150 ng/mL to 0.050 ng/mL). And groα (from 0.080 ng/mL to 0.030 ng/mL). uPAR concentrations in the blood were also reduced by more than 50% at the same dose. JNJ-38877605 mice bearing GTL16 xenografts were orally administered at a dose of 40 mg/kg daily for 72 hours, significantly reduced human plasma levels of IL-8 (from 0.150 ng/mL to 0.050 ng/mL) and GRO alpha (from 0.080 ng/mL to 0.030 ng/mL). uPAR concentrations in the blood were also reduced by more than 50% at the same dose. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.65 ml | 13.25 ml | 26.501 ml |
5 mM | 0.53 ml | 2.65 ml | 5.3 ml |
10 mM | 0.265 ml | 1.325 ml | 2.65 ml |
5 mM | 0.053 ml | 0.265 ml | 0.53 ml |