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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. |
| 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.
| Molecular Weight | 588.56 |
| Formula | C31H26F2N4O6 |
| CAS Number | 1437321-24-8 |
| Purity | >98% |
| Solubility | DMSO 8 mg/mL |
| Storage | at -20°C |
| Related c-Met Products |
|---|
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Bozitinib (PLB-1001; CBT-101) is a highly selective, blood-brain barrier permeable c-MET kinase inhibitor. |
| Glumetinib
Glumetinib, also known as SCC244, is a novel, potent and highly selective inhibitor of c-Met with an IC50 of 0.42 nM. |
| NPS-1034
NPS-1034 is a dual inhibitor of Axl and MET with IC50 values of 10.3 and 48 nM, respectively. |
| Savolitinib (Volitinib)
Savolitinib (volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase. |
| AMG 337
AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor. |
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