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JNJ-38877605

JNJ-38877605

Item no.	S1114-100
Manufacturer	Selleckchem
CASRN	943540-75-8
Amount	100 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 ml 2 mg 200 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Neuroinflammation Metabolism Diabetes Glucose Homeostasis Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Skin Cancer Bladder Cancer Breast Cancer
Type	Inhibitors
Specific against	other
Smiles	CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	943540-75-8'
Similar products	JNJ-38877605
Available
Manufacturer - Targets	MET
Storage Conditions	2 years -80 in solvent
Molecular Weight	377, 35
Administration	Administered via p.o.
Animal Models	GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks, for determination of uPAR and IL-6) of 6-week-old immunodeficient nu/nu female mice on Swiss CD1 background.
Clinical Trials	JNJ-38877605 is currently in Phase I clinical trials in patients with Neoplasms.
Dosages	<=40 mg/kg/day
Formulation	JNJ-38877605 is dissolved in PBS.
IC50	4 nM [1], 4 nM [1], 4 nM [1], 4 nM [1], 4 nM [1], 4 nM [1]
In vitro	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. [1] 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. [2] A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. [3]
In vivo	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 GROalpha (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. [3]
Solubility (25C)	DMSO 15 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	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.
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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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

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S1114-100-datasheet.pdf

S1114-100-safety-datasheet.pdf