An ATP-competitive inhibitor of Met kinase (IC50 = 4 nM); at least 600-fold selective for Met in a panel of ~250 tyrosine and serine-threonine kinases; inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression; sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model at 50 mg/kgp; reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model at 20 mg/kg

JNJ-38877605 – 50 mg

Brand:
Cayman
CAS:
943540-75-8
Storage:
-20
UN-No:
Non-Hazardous - /

JNJ-38877605 is an ATP-competitive inhibitor of Met kinase (IC50 = 4 nM).{46502} It is at least 600-fold selective for Met in a panel of approximately 250 tyrosine and serine-threonine kinases. JNJ-38877605 inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression.{46503} The efficacy of JNJ-38877605 against MET-amplified cells decreases in the presence of increasing concentrations of recombinant human hepatocyte growth factor (HGF). JNJ-38877605 (50 mg/kg) sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model.{46504} It reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model when administered at a dose of 20 mg/kg.{46505}  

 

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Description

An ATP-competitive inhibitor of Met kinase (IC50 = 4 nM); at least 600-fold selective for Met in a panel of ~250 tyrosine and serine-threonine kinases; inhibits the growth of cancer cell lines with MET gene amplification (IC50s = 11-50 nM) but has no effect on the growth of control cells with normal MET gene copy number or no MET expression; sensitizes tumors to radiotherapy in U251 glioma and MDA-MB-231 breast cancer mouse xenograft models and increases apoptosis in irradiated tumors in the MDA-MB-231 mouse xenograft model at 50 mg/kgp; reduces tumor size by 6-fold and the number of blood vessels in tumors by 80% in an RU-P melanoma mouse xenograft model at 20 mg/kg

Formal name: 6-[difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]-quinoline

Synonyms: 

Molecular weight: 377.4

CAS: 943540-75-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling

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