ChemicalBook--->CAS DataBase List--->943540-75-8

943540-75-8

943540-75-8 Structure

943540-75-8 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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;
Spectrum DetailBack Directory
[Spectrum Detail]

J&J Ex-61(943540-75-8)1HNMR
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