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CEP-40783 (RXDX-106) is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively. CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing. In 3/5 (60%) of the tumor models, CEP-40783 shows in vivo efficacy, including tumor regressions, significantly superior to that achieved with an optimal regimen of paclitaxel. In 4/4 (100%) of the erlotinib-insensitive tumor models, CEP-40783 demonstrates significant efficacy (66 to 118% TGI) compared to the control group at the 30 mg/kg dose.
| Cell Experiment | |
|---|---|
| Cell lines | 3T3 cells |
| Preparation method | 3T3 cells expressing Tyro3, Axl, or Mer are incubated with vehicle alone or CEP-40783 for 30 minutes, and receptor phosphorylation is monitored. |
| Concentrations | 0.25, 1, 2.5, 10, 25, 100, 250 nM |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | SCID Beige mice |
| Formulation | |
| Dosages | 30 mg/kg |
| Administration | p.o. |
| Molecular Weight | 588.56 |
| Formula | C31H26F2N4O6 |
| CAS Number | 1437321-24-8 |
| Solubility (25°C) | DMSO 4 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 |
|---|
| 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. |
| BMS 794833
BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor. |
| 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. |
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