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JNJ-38877605

In stock
Catalog No.
A5092
C-Met inhibitor,ATP-competitive
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$116.00
In stock
5mg
$70.00
In stock
25mg
$300.00
In stock
100mg
$800.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Background

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].

Clinical trial: A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.

Reference:
[1] PereraT, L avrijssenT, Janssens B, et al.  JNJ-38877605: a selective Met kinase inhibitor inducing
regression of Met-driven tumor models.  Presented at the 99th AACR Annual Meeting; 2008 Apr 12 -16;

Chemical Properties

StorageStore at -20°C
M.Wt377.35
Cas No.943540-75-8
FormulaC19H13F2N7
Solubility≥18.85mg/mL in DMSO, ≥3.25 mg/mL in EtOH with ultrasonic, <2.47 mg/mL in H2O
Chemical Name6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline
SDFDownload SDF
Canonical SMILESCN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description JNJ-38877605 is an ATP-competitive inhibitor of c-Met with an IC50 value of 4 nM.
Targets c-Met          
IC50 4 nM          

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