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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.
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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 |
| Related FAK Products |
|---|
| PF-562271
PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively. |
| PF-573228
PF-573228 is an ATP-competitive inhibitor of FAK with IC50 of 4 nM, ~50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. |
| PF-00562271
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. |
| Defactinib
Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor, with potential antiangiogenic and antineoplastic activities. |
| PND-1186
PND-1186 (VS-4718) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. |
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