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JNJ-38877605

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Catalog No. T6095Cas No. 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.

JNJ-38877605

JNJ-38877605

🥰Excellent
Purity: 98.27%
Catalog No. T6095Cas No. 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.
Pack SizePriceAvailabilityQuantity
5 mg$32In Stock
10 mg$51In Stock
25 mg$92In Stock
50 mg$148In Stock
1 mL x 10 mM (in DMSO)$34In Stock
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Purity:98.27%
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight377.35
FormulaC19H13F2N7
Cas No.943540-75-8
SmilesCn1cc(cn1)-c1ccc2nnc(n2n1)C(F)(F)c1ccc2ncccc2c1
Relative Density.1.5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 6 mg/mL (15.9 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6501 mL13.2503 mL26.5006 mL132.5030 mL
5 mM0.5300 mL2.6501 mL5.3001 mL26.5006 mL
10 mM0.2650 mL1.3250 mL2.6501 mL13.2503 mL

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