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JNJ-38877605 is a small-molecule, ATP-competitive inhibitor of the catalytic activity of c-Met. JNJ-38877605 showed f600-fold selectivity for c-Met compared with a panel of f250 diverse tyrosine and serine-threonine kinases and was found to potently inhibit HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In addition, JNJ-38877605 induces regression of U87-MG xenografts in vivo.
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Source | Int J Clin Exp Med (2015). Figure 4. JNJ-38877605 |
| Method | CCK-8 assay | |
| Cell Lines | PC-3 human prostate cancer cells | |
| Concentrations | 0.125 nM, 0.5 nM, 1 nM, 2.5 nM, 5 nM, 10 nM | |
| Incubation Time | 48 h | |
| Results | However, different concentrations of saracatinib, linsitinib and JNJ-38877605 did not inhibit PC-3 cells proliferation after 48 h, high or low concentrations of the three inhibitors did not inhibit PC-3 cells proliferation at all. |
| Cell Experiment | |
|---|---|
| Cell lines | S114, GTL-16, NCI-H441, or BxPC-3 cells |
| Preparation method | Cell Proliferation Assays. S114, GTL-16, NCI-H441, or BxPC-3 cells were seeded in 96-well plates at 9000 cells/well in medium with 10% FBS. After incubation for 48 h in low serum (0.5% FBS, S114; 0.1% FBS, GTL-16, NCI-H441, and BxPC-3), cells were treated with different concentrations of PHA-665752 for 18 h at 37°C. HGF (50 ng/ml) was added for 18 h before BrdUrd for studies involving GTL-16, H441, and BxPC-3. After incubation with BrdUrd labeling reagent for 1 h (Sigma Biochemicals, St. Louis, MO), cells were fixed and BrdUrd incorporation into newly synthesized DNA was assessed using anti-BrdUrd peroxidase-conjugated antibody followed by colorimetric determination at 630 nm. |
| Concentrations | 0~1.25µM |
| Incubation time | 18 h |
| Animal Experiment | |
|---|---|
| Animal models | Female athymic mice bearing S114 or GTL-16 tumor xenografts |
| Formulation | L-lactate (pH 4.8) and 10% polyethylene glycol |
| Dosages | 25 mg/kg a single i.v. dose |
| Administration | via bolus i.v. tail vein injection |
| Molecular Weight | 377.35 |
| Formula | C19H13F2N7 |
| CAS Number | 943540-75-8 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related c-Met Products |
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Zurletrectinib (ICP-723) is a potent tyrosine kinase inhibitor. Zurletrectinib serves as an antineoplastic agent. Zurletrectinib can used for research of TRK-mediated related diseases. |
| ABN401
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. |
| (Z)-Semaxanib
(Z)-Semaxanib is a potent tyrosine kinase inhibitor. |
| MET kinase-IN-2
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. |
| BMS-817378
BMS-817378 is a potent and selective inhibitor of MET with IC50 of 1.7 nM. |
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