JNJ-38877605 943540-75-8

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Molecular Weight:

377.35 JNJ-38877605 is an ATP-Competitive Inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1.


Biological Activity


JNJ-38877605 shows more than 600-fold selectivity for c-Met compared
with more than 200 Other diverse tyrosine and serine-threonine kinases
and also potently inhibits HGF-stimulated and constitutively activated
c-Met phosphorylation in vitro. In EBC1, GTL16,
NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant
reduction of phosphorylation of Met and RON, another key player in
invasive growth. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells.


In mice bearing established GTL16 xenografts, JNJ-38877605, dosed orally
with 40 mg/kg/day for 72 hours, results in a statistically significant
decrease in the plasma levels of human IL-8 (from 0.150 ng/mL to 0.050
ng/mL) and GROα (from 0.080 ng/mL to 0.030 ng/mL). While concentrations
of uPAR in the blood become reduced to more than 50% at the same dose.


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	377.35
Formula	C19H13F2N7
CAS No.	943540-75-8

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	37 mg/mL (98.05 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% propylene glycol, 5% Tween 80, 65% D5W	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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

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Product Categories : Protein Tyrosine Kinase > c-Met Inhibitor