Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM.
 |
Source | J Biol Chem (2011). Figure 8. NVP-TAE226 |
| Method | Western blotting | |
| Cell Lines | HEK293 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 90 min | |
| Results | To test the biological importance of the reciprocal RET-FAK transactivation, established HEK293 cells expressing a constitutively active RET mutant (RET C634R) were treated with the FAK kinase inhibitor NVP-TAE226 |
| Cell Experiment | |
|---|---|
| Cell lines | U87, U87 EGFR, U87 vIII and U251 cells |
| Preparation method | Cell Viability Assay Cell cultures were harvested with 0.05% trypsin and seeded in triplicate at 2 × 104 in 24-well culture plates for 24 h before drug treatment. Culture medium was used for mock treatment. Cells were harvested at the indicated day after treatment, and viable cells were counted using the Vi-cell viability analyzer. |
| Concentrations | 1 and 10 μmol/L |
| Incubation time | 1, 3 and 5 days |
| Animal Experiment | |
|---|---|
| Animal models | U87 and LN229 glioma xenograft Intracranial Animal Model |
| Formulation | 0.5% methylcellulose |
| Dosages | 50 or 75 mg/kg once a day for 5 days and off for 2 days, for a duration of 4 weeks |
| Administration | oral gavage |
| Molecular Weight | 468.94 |
| Formula | C23H25ClN6O3 |
| CAS Number | 761437-28-9 |
| Solubility (25°C) | DMSO 66 mg/mL |
| 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.
| Related FAK Products |
|---|
| Petunidin chloride
Petunidin chloride is an O-methylated anthocyanidin derived from delphinidin. *The compound is unstable in solutions, freshly prepared is recommended. |
| FAK-IN-11
FAK-IN-11 is a FAK inhibitor. |
| ZINC40099027
ZINC40099027 is a FAK activator. |
| FC-11
FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . |
| FAK-IN-9
FAK-IN-9 is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. |
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