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 | |
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Cell lines | gastric cancer cell line (GTL-16) |
Preparation method | cell proliferation assay |
Concentrations | IC50 = 39 nM |
Incubation time |
Animal Experiment | |
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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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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