All AbMole products are for research use only, cannot be used for human consumption.
BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor and it also inhibits Ron (Met family), Axl and Flt-3 with IC50 values <3 nM. BMS-794833 was selective versus a panel of >200 additional RTKs, non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. In cell culture, BMS-794833 inhibited the proliferation of human tumor cell lines containing constitutively activated Met receptor (GTL-16 gastric carcinoma). In vivo, BMS-794833 demonstrated dose-dependent tumor growth inhibition following oral administration in the GTL-16 and L2987 lung carcinoma (Met-insensitive) xenograft models.
| Cell Experiment | |
|---|---|
| Cell lines | gastric cancer cell line (GTL-16) |
| Preparation method | cell proliferation assay |
| Concentrations | IC50 = 39 nM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | U87 glioblastoma model |
| Formulation | |
| Dosages | 25mg/kg |
| Administration | |
| Molecular Weight | 468.84 |
| Formula | C23H15ClF2N4O3 |
| CAS Number | 1174046-72-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related c-Met Products |
|---|
| AMG-208
AMG-208 is a potent small molecular inhibitor c-Met with an IC50 of 9.3 nM. AMG-208 is also a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity. |
| BMS-777607
BMS-777607 is a selective and potent small-molecule met kinase inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively. |
| AMG-458
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively. |
| XL-184
Cabozantinib (XL184, BMS-907351) is a small molecule inhibits multiple receptor tyrosine kinases, specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM for VEGFR2 and Met respectively. |
| Foretinib
Foretinib (XL880, GSK1363089) is a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2 (VEGFR2) with IC50 value of 0.4 nM for c-MET. |
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