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JNJ-38877605

Catalog No. T6095   CAS 943540-75-8

JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.

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JNJ-38877605 Chemical Structure
JNJ-38877605, CAS 943540-75-8
Pack Size Availability Price/USD Quantity
2 mg In stock $ 34.00
5 mg In stock $ 53.00
10 mg In stock $ 85.00
25 mg In stock $ 153.00
50 mg In stock $ 247.00
100 mg In stock $ 405.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Purity: 98.27%
Purity: 97.15%
Purity: 97.04%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
Targets&IC50 c-Met:4 nM
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. 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 vivo In mice bearing established GTL16 xenografts, JNJ-38877605 (40 mg/kg/day, p.o., total 3day) results in a statistically marked decrease in the plasma levels of human IL-8 (0.150-0.050 ng/mL) and GROα (0.080-0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose.
Animal Research 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 immuno-deficient nu/nu female mice on Swiss CD1 background. Formulation: JNJ-38877605 is dissolved in PBS. Dosages: ≤40 mg/kg/day. Administration: Administered via p.o.
Molecular Weight 377.35
Formula C19H13F2N7
CAS No. 943540-75-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 35 mg/mL (92.8 mM)

TargetMolReferences and Literature

1. De Bacco F, et al. J Natl Cancer Inst. 2011 Apr, 103(8), 645-661. 2. Torti D, et al. Int J Cancer. 2012, 130(6), 1357-1366.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max

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Keywords

JNJ-38877605 943540-75-8 Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor inhibit JNJ38877605 JNJ 38877605 inhibitor

 

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