| Identification | Back Directory | [Name]
J&J Ex-61 | [CAS]
943540-75-8 | [Synonyms]
CS-43
J&J Ex-61
JNJ-38877605
JNJ-33877605
JNJ 38877605 NEW
J&J Ex-61 USP/EP/BP
JNJ38877605; JNJ-38877605
6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[3,4-f]...
6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[3,4-f]pyridazin-3-yl]methyl]quinoline
6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
6-(Difluoro(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]-triazolo[4,3-b]pyridazin-3-yl)methyl)quinolin
Quinoline, 6-[difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]-
JNJ 38877605
6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
6-[Difluoro[6-(1-methyl-1H-pyrazol-4-yl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline JNJ 38877605 | [Molecular Formula]
C19H13F2N7 | [MDL Number]
MFCD11977274 | [MOL File]
943540-75-8.mol | [Molecular Weight]
377.357 |
| Chemical Properties | Back Directory | [density ]
1.50 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥3.25 mg/mL in EtOH with ultrasonic | [form ]
Powder | [pka]
3.92±0.10(Predicted) | [color ]
Off-white to light yellow | [CAS DataBase Reference]
943540-75-8 |
| Hazard Information | Back Directory | [Uses]
JNJ-38877605 is a potent inhibitor of c-Met catalytic activity. Selective over other tyrosine and serine-threonine kinases (600-fold selectivity). Ability to block constitutive or HGF-stimulated phosphorylation of c-Met demonstrated in vitro. JNJ 38877605 reduces radiation-induced invasion, apoptosis and proliferation of cancer cells in vitro. | [Definition]
ChEBI:6-[difluoro-[6-(1-methyl-4-pyrazolyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline is a member of quinolines. | [Biological Activity]
jnj-38877605 is a small-molecule atp-competitive inhibitor of the catalytic activity of c-met.extensive evidence that c-met signaling is involved in the progression and spread of several cancers and an enhanced understanding of its role in disease have generated considerable interest in c-met and hgf asmajor targets in anti-cancer drug development. | [in vitro]
jnj-38877605 showed ~600-fold selectivity for c-met compared with a panel of ~250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit hgf-stimulated and constitutively activated c-met phosphorylation in vitro [1]. | [in vivo]
jnj-38877605 showed excellent oral bioavailability approaching 100% in all examined species. in addition, jnj-38877605 in a single dose was observed toinhibit met phosphorylation in tumor xenografts for up to16 h. inhibition of met phosphorylation was associated withdose-dependent tumor growth inhibition using a range of oral dosing regimens [2]. | [target]
c-Met | [storage]
Store at -20°C | [References]
[1] pererat, l avrijssent, janssens b, et al. jnj-38877605: a selective met kinase inhibitor inducingregression of met-driven tumor models. presented at the 99th aacr annual meeting; 2008 apr 12 -16; |
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