JNJ-38877605
Cat. No. :YN440401
CAS No. :943540-75-8
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Product Name: | JNJ-38877605 |
CAS NO.: | 943540-75-8 |
Chemical Name: | |
Synonyms: | |
Molecular Weight: | 377.35 |
Molecular Formula: | C₁₉H₁₃F₂N₇ |
SMILES: | FC(F)(C1=NN=C2C=CC(C3=CN(C)N=C3)=NN21)C4=CC5=C(N=CC=C5)C=C4 |
Storage: | Please store the product under the recommended conditions in the Certificate of Analysis. |
Transportation: | Room temperature in continental US; may vary elsewhere. |
Description: | JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4nM, 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 (500nM) 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, 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 . |
IC50&Target: | |
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References: |
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