J&J Ex-61 Chemical Properties

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)

CAS DataBase Reference

943540-75-8

J&J Ex-61 Usage And Synthesis

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

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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